1,588 results match your criteria Medicinal Chemistry[Journal]


Chemistry, Alpha-glucosidase and Radical Scavenging Properties of Uranyl(VI) Hydrazide Complexes.

Med Chem 2019 Feb 12. Epub 2019 Feb 12.

Department of Chemistry, University of Karachi, Karachi 75270. Pakistan.

Background: Antioxidant, anti-inflammatory, antiviral and antitumoral activities among others are essential characteristics in the development of novel therapeutic compounds. Acid hydrazides can form complexation with certain metal ions that positively enhances these biological characteristics.

Objective: Five new complexes of uranium with hydrazide ligands were synthesized at room temperature. Read More

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http://dx.doi.org/10.2174/1573406415666190213101044DOI Listing
February 2019

Cytotoxicity, pro-apoptotic activity and in silico studies of dithiocarbamates and their structure based design and SAR Studies.

Med Chem 2019 Feb 11. Epub 2019 Feb 11.

Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad-22060. Pakistan.

Background: Cancer is a far reaching and lethal but cureable disease. Reasearchers have investigated numerous anticancer agents with only few commercialy available effective drugs which are very costly.

Objective: Herein we report the synthesis , characterization and anti cancer assays of a series of novel dithiocarbamates derivatives. Read More

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http://dx.doi.org/10.2174/1573406415666190211162013DOI Listing
February 2019

Antibacterial Evaluation of Novel Substituted Cycloheptaindoles in Staphylococcus and Enterococcus strains.

Med Chem 2019 Feb 8. Epub 2019 Feb 8.

Institute of Biochemistry, Ernst-Moritz-Arndt University Greifswald, Felix-Hausdorff-Str. 4, 17487 Greifswald. Germany.

Background: Due to emerging resistances against antibiotics there is a strong need to find novel antibacterial agents with a novel structure to prevent early resistance developments.

Objective: Bisindole compounds with antibacterial activities which formally result from the reaction of an aldehyde with indole motivated to investigate the reaction of a dialdehyde and indole to give novel structures with potential antibacterial activities.

Method: Compounds were yielded by chemical synthesis and purified using column chromatography. Read More

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http://dx.doi.org/10.2174/1573406415666190208170126DOI Listing
February 2019

Antiglycation activity of triazole Schiff's bases against fructose-mediated glycation: In vitro and in silico study.

Med Chem 2019 Feb 11. Epub 2019 Feb 11.

Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270. Pakistan.

Background: Advanced glycation end products (AGEs) are known to be involved in pathophysiology of diabetic complications, neurodegenerative diseases, and aging. Preventing the formation of AGEs can be helpful in the management of these diseases.

Objective: Two classes of previously synthesized traizole Schiff's bases (4H-1,2,4-triazole-4-Schiff's bases 1-14, and 4H-1,2,4-triazole-3-Schiff's bases 15-23) were evaluated for their in vitro antiglyaction activity. Read More

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http://dx.doi.org/10.2174/1573406415666190212105718DOI Listing
February 2019

The effects of trifluoromethylated derivatives on prostaglandin E2 and thromboxane A2 production in human leukemic U937 macrophages.

Med Chem 2019 Feb 8. Epub 2019 Feb 8.

Department of Physiology and Pharmacology "Vittorio Erspamer", La Sapienza University, P.le Aldo Moro 5, I-00185 Rome. Italy.

Background: Convenient approach to modulation of the inflammation is influence on production of inflammatory mediators - eicosanoids, generated in arachidonic acid (AA) metabolism. Common therapeutic activity of non-steroidal anti-inflammatory drugs (NSAID), such as aspirin, includes inhibition of two crucial enzymes of AA metabolism - cyclooxygenase-1 and -2 (COX-1/2), with certain risk for gastrointestinal and renal intolerance. Ever since enrolment of COX-2, particularly overabundance of its main products prostaglandin E2 (PGE2) and thromboxane A2 (TXA2) in numerous pathological processes was recognized, it became significant therapeutic target. Read More

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http://dx.doi.org/10.2174/1573406415666190208150253DOI Listing
February 2019

Structure Activity Relationship of 4-Amino-2-thiopyrimidine Derivatives as Platelet Aggregation Inhibitors.

Med Chem 2019 Feb 8. Epub 2019 Feb 8.

Unità di Medicina III, Azienda Ospedaliera San Paolo, Dipartimento di Medicina Chirurgia e Odontoiatria, Università di Milano, Via di Rudinì 8, I-20142 Milano. Italy.

Background: Platelet aggregation plays a pathogenic role in the development of arterial thrombi, which are responsible for common diseases caused by thrombotic arterial occlusion, such as myocardial infarction and stroke. Much efforts is directed toward developing platelet aggregation inhibitors that act through several mechanisms: the main antiplatelet family of COX-inhibitors, phosphodiesterase inhibitors, and thrombin inhibitors. Recently, the important role in the platelet aggregation of adenosine diphosphate (ADP)-activated P2Y12 and P2Y1 receptors, G-protein coupled receptors of the P2 purinergic family, has emerged, and their inhibitors are explored as potential therapeutic antithrombotics. Read More

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http://dx.doi.org/10.2174/1573406415666190208124534DOI Listing
February 2019

Design, Synthesis, and Anti-bacterial Activity of Novel Deoxycholic Acid-Amino Alcohol Conjugates.

Med Chem 2019 Feb 6. Epub 2019 Feb 6.

Chemistry Department, Centre for Engineering and Enterprise Institute of Advanced Research, Koba Institutional Area Gandhinagar, Gujarat, 382426. India.

Background: Numerous of synthetic bile acid derivatives have been recognized for its various biological activities. Among these, bile acid amides have emerged as an attractive antibacterial agent. We herein illustrate the synthesis and antibacterial evaluation of deoxycholic acid-amino alcohols conjugates. Read More

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http://dx.doi.org/10.2174/1573406415666190206231002DOI Listing
February 2019

Target Based Virtual Screening of New Leads Inhibitor against Bacterial Cell Division Protein FtsZ for the Discovery of Antibacterial Agents.

Med Chem 2019 Feb 6. Epub 2019 Feb 6.

Depatment of Genetics, Maharshi Dayanand University, Rohtak-124001, Haryana. India.

Background: Staphylococus epidermidis coagulase negative and gram positive streptococci have emerge as major nosocomial pathogens associated with infection of implanted medical devices and dandruff in human scalp. S. epidermidis filamenting temperature-sensitive mutant Z (FtsZ) gene encoded FtsZ protein that assembles at future bacterial cell division site that form Z-ring structure. Read More

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http://dx.doi.org/10.2174/1573406415666190206233448DOI Listing
February 2019
1 Read

Polyethylene glycol acts as a mechanistic stabilizer of L-asparaginase: a computational probing.

Med Chem 2019 Feb 6. Epub 2019 Feb 6.

Food Protectants and Infestation Control Dept., CSIR-Central Food Technological Research Institute Mysore - 570 020. India.

L-asparaginase (L-ASN) is an anti-cancer enzyme therapeutic drug that exerts cytotoxicity via inhibition of protein synthesis through depletion of L-asparagine in the tumour microenvironment. The therapeutic performance of the native drug is partial due to the associated instability, reduced half-life and immunogenic complications. In this study, we report the modification of recombinant L-asparaginase with PEG and an integrated computational strategy to probe the PEGylation in the protein to understand the biological stability/activity imparted by PEG. Read More

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http://dx.doi.org/10.2174/1573406415666190206232816DOI Listing
February 2019

Structure-activity relationship study on therapeutically relevant EGFR double mutant inhibitors.

Med Chem 2019 Feb 6. Epub 2019 Feb 6.

Bioinformatics Division, ICMR-National Institute of Cancer Prevention and Research, I-7, Sector-39, Noida-201301. India.

Background: EGFR is a clinically approved drug target in cancer. The first generation tyrosine kinase inhibitors targeting L858R mutated EGFR are routinely used to treat non-small cell lung cancer (NSCLC). However, the presence of a secondary mutation (T790M) tenders these inhibitors ineffective and thus results in the relapse of the disease. Read More

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http://dx.doi.org/10.2174/1573406415666190206204853DOI Listing
February 2019
1 Read

Synthesis, design and antiplasmodial evaluation of sulfoximine-triazole hybrids as potential antimalarial prototypes.

Med Chem 2019 Feb 6. Epub 2019 Feb 6.

Department of Chemistry, Faculty of Science, University of Johannesburg, Johannesburg. South Africa.

Background: Malaria, caused by the deadly Plasmodium falciparum strain, claims the lives of millions of people annually. The emergence of drug-resistant strains of P. falciparum to the artemisinin-based combination therapy (ACT), the last line of defense against malaria, is worrisome and urges for the development of new chemo-types with new mode of actions. Read More

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http://dx.doi.org/10.2174/1573406415666190206232308DOI Listing
February 2019

Synthesis, Antimicrobial Evaluation and Molecular Docking of Some Potential 2,6-disubstituted 1H-Benzimidazoles; Non-Classical Antifolates.

Med Chem 2019 Feb 6. Epub 2019 Feb 6.

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Faculty of Pharmaceutical Sciences, Shivaji University, Kolhapur (MS). India.

Background: Dihydrofolate reductase is one of the important enzymes for thymidylate and purine synthesis in micro-organisms. A large number of drugs have been designed to inhibit microbial DHFR but over the period of time some drugs have developed resistance and cross reactivity towards the enzyme. Over the past few decades, benzimidazoles, triazoles and their derivatives have been grabbing the attention of the synthetic chemists for their wide gamut of antibacterial and antifungal activities targeting microbial protein DHFR. Read More

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http://dx.doi.org/10.2174/1573406415666190206231555DOI Listing
February 2019

Synthesis, Anticancer Evaluation and Synergistic Effects with cisplatin of Novel Palladium Complexes: DNA, BSA Interactions and Molecular Docking Study.

Med Chem 2019 Jan 27. Epub 2019 Jan 27.

University of Kragujevac, Faculty of Science, Department of Chemistry, Radoja Domanovića 12, 34000 Kragujevac. Serbia.

Background: In order to discover new agents for chemotherapy with improved properties related to existing and bearing in mind the fact that some Pd complexes possess better antitumor activity and exhibit less kidney toxicity comparing to cisplatin, series of novel square-planar palladium(II) complexes [Pd (L)2] (3a-f) with O,O bidentate ligands [L = ethyl 2-hydroxy-alkyl(aryl)-4-oxo-2-butenoate] were synthesized.

Methods: All complexes were characterized by spectral (UV-Vis, IR, NMR, ESI-MS) and X-ray analysis and examined for their cytotoxic effect on human cancer cell lines HeLa and MDA-MB 231 and normal fibroblasts (MRC-5). Fluorescence spectroscopic method was used for investigations of the interactions between CT-DNA or bovine serum albumin (BSA) and complex 3c. Read More

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http://dx.doi.org/10.2174/1573406415666190128095732DOI Listing
January 2019

Synthesis of New Hydrazone Derivatives and Evaluation of their Efficacy as Proliferation Inhibitors in Human Cancer Cells.

Med Chem 2019 Jan 27. Epub 2019 Jan 27.

Department of Molecular and Cellular Biology, Wroclaw Medical University, Borowska 211A, 50-556 Wroclaw. Poland.

Background: Hydrazine-hydrazones represent a group of bioactive compounds that display antibacterial, anti-inflammatory, antiviral or anticancer activities.

Objective: In this study, we designed new derivative compounds from groups of hydrazones.

Method: The group of new derivatives was evaluated by the viability assay in human cancer and normal cells. Read More

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http://dx.doi.org/10.2174/1573406415666190128100524DOI Listing
January 2019
1 Read

The Inhibition of Polysialyltranseferase ST8SiaIV through Heparin binding to Polysialyltransferase Domain (PSTD).

Med Chem 2018 Dec 17. Epub 2018 Dec 17.

Life Science and technology College, Guangxi University, Nanning, Guangxi, 530004 . China.

Background: The polysialic acid (polySia) is a unique carbohydrate polymer produced on the surface of neuronal cell adhesion molecule (NCAM) in a number of cancer cells, and strongly correlates with the migration and invasion of tumor cells and with aggressive, metastatic disease and poor clinical prognosis in the clinic. Its synthesis is catalyzed by two polysialyltransferases (polySTs), ST8SiaIV (PST) and ST8SiaII (STX). Selective inhibition of polySTs, therefore presents a therapeutic opportunity to inhibit tumor invasion and metastasis due to NCAM polysialylation. Read More

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http://www.eurekaselect.com/168414/article
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http://dx.doi.org/10.2174/1573406415666181218101623DOI Listing
December 2018
7 Reads
1.387 Impact Factor

pLoc_bal-mEuk: predict subcellular localization of eukaryotic proteins by general PseAAC and quasi-balancing training dataset.

Med Chem 2018 Dec 17. Epub 2018 Dec 17.

Gordon Life Science Institute, Boston, MA 02478. United States.

Objective: Information of protein subcellular localization is crucially important for both basic research and drug development. With explosive growth of protein sequences discovered in the post-genomic age, it is highly demanded to develop powerful bioinformatics tools for timely and effectively identifying their subcellular localization purely based on the sequence information alone. Recently, a predictor called "pLoc-mEuk" was developed for identifying the subcellular localization of eukaryotic proteins. Read More

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http://dx.doi.org/10.2174/1573406415666181218102517DOI Listing
December 2018
1.387 Impact Factor

Synthesis, Plasmodium falciparum Inhibitory Activity, Cytotoxicity and Solubility of N2,N4-Disubstituted Quinazoline-2,4-diamines.

Med Chem 2018 Dec 18. Epub 2018 Dec 18.

Biomedical Engineering, Faculty of Engineering, King Mongkut's Institute of Technology Ladkrabang, Bangkok. Thailand.

Background: Despite the development of extensive control strategies and treatment options, approximately 200 million malaria cases, leading to approximately 450,000 deaths, were reported in 2015. Due to issue of disease resistance, additional drug development efforts are needed to produce new, more effective treatments. Quinazoline-2,4-diamines were identified as anti-parasitic compounds over three decades ago and have remained of interest to date in industry and academia. Read More

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http://dx.doi.org/10.2174/1573406415666181219100307DOI Listing
December 2018
2 Reads

The Multiple Applications and Possible Mechanisms of the Hyperbaric Oxygenation Therapy.

Med Chem 2018 Dec 18. Epub 2018 Dec 18.

Department of Respiratory Medicine, the People's Hospital of Guangxi Zhuang Autonomous Region, Nanning, Guangxi 530021. China.

Hyperbaric Oxygenation Therapy (HBOT) is used as adjunctive method for multiple diseases. The method meets the routine treating and is non-invasive, as well as provides 100% pure oxygen (O2) which is at above-normal atmospheric pressure in a specialized chamber. It is well known that in the condition of O2 deficiency, it will induce a series of adverse events. Read More

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http://dx.doi.org/10.2174/1573406415666181219101328DOI Listing
December 2018
1 Read

Structural variability in the RLR-MAVS pathway and sensitive detection of viral RNAs.

Authors:
Qiu-Xing Jiang

Med Chem 2018 Dec 18. Epub 2018 Dec 18.

Department of Microbiology and Cell Science, University of Florida 1355 Museum Drive, PO Box 110700, Gainesville, FL 32611. United States.

Cells need high-sensitivity detection of non-self molecules in order to fight against pathogens. These cellular sensors are thus of significant importance to medicinal purposes, especially for treating novel emerging pathogens. RIG-I-like receptors (RLRs) are intracellular sensors for viral RNAs (vRNAs). Read More

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http://dx.doi.org/10.2174/1573406415666181219101613DOI Listing
December 2018

Synthesis, Molecular Modelling and Biological Studies of 3-hydroxy-pyrane-4-one and 3-hydroxy-pyridine-4-one Derivatives as HIV-1 Integrase Inhibitors.

Med Chem 2018 Dec 18. Epub 2018 Dec 18.

Department of Chemistry, Faculty of Sciences, University of Isfahan, 81746-73441 Isfahan. Iran.

Background: Despite the progresses in the discovery of antiretroviral compounds for treating HIV-1 infection by targeting HIV integrase (IN), a promising and well-known drug target against HIV-1, there is a growing need to increase the armamentarium against HIV, for avoiding the drug resistance issue.

Objective: To develop novel HIV-1 IN inhibitors, a series of 3-hydroxy-pyrane-4-one (HP) and 3-hydroxy-pyridine-4-one (HPO) derivatives have been rationally designed and synthesized.

Method: To provide a significant characterization of the novel compounds, an in-depth computational analysis was performed using a novel HIV-1 IN/DNA binary 3D-model for investigating the binding mode of the newly conceived molecules in complex with IN. Read More

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http://www.eurekaselect.com/168447/article
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http://dx.doi.org/10.2174/1573406415666181219113225DOI Listing
December 2018
10 Reads
1.387 Impact Factor

Discovery of N-phenyl-4-(1H-pyrrol-3-yl)pyrimidin-2-amine derivatives as potent Mnk2 inhibitors: design, synthesis, SAR analysis, and evaluation of in vitro anti-leukaemic activity.

Med Chem 2018 Dec 18. Epub 2018 Dec 18.

Centre for Drug Discovery and Development, Cancer Research Institute, School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia 5001. Australia.

Background: Aberrant expression of eukaryotic translation initiation factor 4E (eIF4E) is common in many types of cancer including acute myeloid leukaemia (AML). Phosphorylation of eIF4E by MAPK-interacting kinases (Mnks) is essential for the eIF4E-mediated oncogenic activity. As such, the pharmacological inhibition of Mnks can be an effective strategy for the treatment of cancer. Read More

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http://dx.doi.org/10.2174/1573406415666181219111511DOI Listing
December 2018
14 Reads

Inhibition of α-amylase activity by Zn2+: insights from spectroscopy and molecular dynamics simulations.

Med Chem 2018 Dec 16. Epub 2018 Dec 16.

College of Life Science and Technology, Guangxi University, Nanning, Guangxi, 530004 . China.

Background: Inhibition of α-amylase activity is an important strategy in the treatment of diabetes mellitus. An important treatment for diabetes mellitus is to reduce the digestion of carbohydrates and blood glucose concentrations. Inhibiting the activity of carbohydrate-degrading enzymes such as α-amylase and glucosidase significantly decreases the blood glucose level. Read More

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http://dx.doi.org/10.2174/1573406415666181217114101DOI Listing
December 2018
1.387 Impact Factor

pLoc_bal-mVirus: predict subcellular localization of multi-label virus proteins by PseAAC and IHTS treatment to balance training dataset.

Med Chem 2018 Dec 16. Epub 2018 Dec 16.

Center for Informational Biology, University of Electronic Science and Technology of China, Chengdu, 610054. China.

Objective: Knowledge of protein subcellular localization is vitally important for both basic research and drug development. Facing the avalanche of protein sequences emerging in the post-genomic age, it is urgent to develop computational tools for timely and effectively identifying their subcellular localization based on the sequence information alone. Recently, a predictor called "pLoc-mVirus" was developed for identifying the subcellular localization of virus proteins. Read More

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http://dx.doi.org/10.2174/1573406415666181217114710DOI Listing
December 2018
1.387 Impact Factor

New Quinazoline-Sulfonylurea Conjugates: Design, Synthesis and Hypoglycemic Activity.

Med Chem 2018 12 7. Epub 2018 Dec 7.

Department of Biochemistry, Faculty of Science, Ain Shams University, Cairo. Egypt.

Background: Sulphonylureas are the oldest and commonly used to treat diabetic patients, but its efficacy declines by time. It was reported that quinazoline nucleus exhibits a potent hypoglycemic effect in diabetic animal models.

Objective: The current study aimed to synthesize new quinazoline-sulfonylurea conjugates and evaluate their hypoglycemic effects in alloxan-induced diabetic rats. Read More

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http://dx.doi.org/10.2174/1573406415666181208104543DOI Listing
December 2018

Benzoylthioureas: Design, Synthesis and Antimycobacterial Evaluation.

Med Chem 2018 Dec 7. Epub 2018 Dec 7.

Departamento de Química, Centro de Ciências Exatas, Universidade Estadual de Londrina, Rodovia Celso Garcia Cid (PR 445), Km 380, Campus Universitário, Londrina - PR, 86057-970. Brazil.

Background: New drugs and strategies to treat tuberculosis (TB) are urgently needed. In this context, thiourea derivatives have a wide range of biological activities, including anti-TB. This fact can be illustrated with the structure of isoxyl, an old anti-TB drug, which have a thiourea as pharmacophore group. Read More

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http://dx.doi.org/10.2174/1573406415666181208110753DOI Listing
December 2018
3 Reads

Evaluation of Cytotoxic Potentials of Some Isoindole-1,3-Dione Derivatives on HeLa, C6 and A549 Cancer Cell Lines.

Med Chem 2018 Dec 5. Epub 2018 Dec 5.

Department of Chemistry, Faculty of Sciences, Atatürk University, 25240 Erzurum. Turkey.

Background: Norcantharimides are known as norcantharidine derivatives and contain an isoindole skeleton structure. Isoindole derivatives have positively effect on inflammatory pathologies including cancers.

Objective: Considering this information, firstly, isoindole derivatives containing different functional groups 4-13 have been synthesized from 2-alkyl/aryl-3a,4,7,7a-tetrahydro-1H-isoindole-1,3(2H)-dione. Read More

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http://dx.doi.org/10.2174/1573406415666181206115638DOI Listing
December 2018
2 Reads

Synthesis, Characterization, Antibacterial and Antioxidant Potency of N-Substituted-2-Sulfanylidene-1,3-Thiazolidin-4-one Derivatives and QSAR Study.

Med Chem 2018 Dec 5. Epub 2018 Dec 5.

Faculty of Agrobiotehnical Sciences Osijek, Josip Juraj Strossmayer University of Osijek, Osijek. Croatia.

Background: Rhodanine is known for its potential and important role in the medicinal chemistry since its derivatives exhibit a wide range of pharmacological activities such as antibacterial, antifungal, antidiabetic, antitubercular, anti-HIV, antiparasitic, antioxidant, anticancer, anti-proliferative and anthelmintic agents.

Objectives: Since N-substituted rhodanine synthons are rarely commercially available, it is desirable to develop a straight forward synthetic approach for the synthesis of these key building blocks. The objective was to synthesize a series of rhodanine derivatives and to investigate their antimicrobial and antioxidant activity. Read More

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http://www.eurekaselect.com/168098/article
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http://dx.doi.org/10.2174/1573406415666181205163052DOI Listing
December 2018
3 Reads

The Substantial Improvement of Amphotericin B Selective Toxicity upon Modification of Mycosamine with Bulky Substituents.

Med Chem 2018 Dec 2. Epub 2018 Dec 2.

Department of Pharmaceutical Technology and Biochemistry, Faculty of Chemistry, Gdań sk University of Technology, 11/12 Narutowicza St., 80-233 Gdańsk. Poland.

Background It is assumed that the unfavorable selective toxicity of an antifungal drug Amphotericin B (AmB) can be improved upon chemical modification of the antibiotic molecule. Objective The aim of this study was verification of the hypothesis that introduction of bulky substituents at the amino sugar moiety of the antibiotic may result in diminishment of mammalian in vitro toxicity of thus prepared AmB derivatives. Methods Twenty eight derivatives of AmB were obtained upon chemical modification of the amino group of mycosamine residue. Read More

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http://dx.doi.org/10.2174/1573406415666181203114629DOI Listing
December 2018
1 Read

Synthesis and biological studies of new multifunctional curcumin platforms for anticancer drug delivery.

Med Chem 2018 Dec 2. Epub 2018 Dec 2.

Department of Chemical Sciences, Ariel University, Ariel, 40700. Israel.

Background: Scientists have extensively investigated curcumin, yielding many publications on treatments of cancer. Numerous derivatives of curcumin were synthesized, evaluated for their anti-oxidant and free-radical scavenging, SAR, ADME properties and tested in anticancer applications.

Objective: We decided to exploit curcumin as a bioactive core platform for carrying anticancer drugs, which likely possesses a carboxyl moiety for potential linkage to the carrier for drug delivery. Read More

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http://dx.doi.org/10.2174/1573406415666181203112220DOI Listing
December 2018
1 Read

Efficacy of novel Schiff base derivatives as antifungal compounds in combination with approved drugs against Candida albicans.

Med Chem 2018 Dec 2. Epub 2018 Dec 2.

Department of Chemistry, Jamia Millia Islamia (Central University), New Delhi-110025. India.

Background: The increasing incidence of fungal infections, especially caused by Candida albicans, and their increasing drug resistance has drastically increased in recent years. Therefore, not only new drugs but alternative treatment strategies are promptly required.

Methods: We previously reported on the synergistic interaction of some azole and non-azole compounds with fluconazole for combination antifungal therapy. Read More

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http://dx.doi.org/10.2174/1573406415666181203115957DOI Listing
December 2018

Identification, Prediction and Data Analysis of Non Coding RNAs: A Review.

Med Chem 2018 Oct 15. Epub 2018 Oct 15.

Department of Mathematics, Faculty of Sciences, University of Isfahan, Isfahan. Iran.

Background: Non coding RNAs (ncRNAs) which play an important role in various cellular processes are important in medicine as well as drug design strategies. Different studies have shown that ncRNAs are dis-regulated in cancer cells and play an important role in human tumorigenesis. Therefore, it is important to identify and predict such molecules by experimental and computational methods, respectively. Read More

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http://www.eurekaselect.com/166269/article
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http://dx.doi.org/10.2174/1573406414666181015151610DOI Listing
October 2018
3 Reads

Design, synthesis and anxiolytic activity evaluation of N-acyl-tryptophanyl-containing dipeptides, potential TSPO ligands.

Med Chem 2018 Nov 19. Epub 2018 Nov 19.

Federal State Budgetary Institution "Research Zakusov Institute of Pharmacology" (FSBI "Zakusov Institute of Pharmacology"). Russian Federation.

Background: The 18 kDa translocator protein (TSPO), previously known as the peripheral-type benzodiazepine receptor, plays a key role for synthesis of neurosteroids by promoting transport of cholesterol from the outer to the inner mitochondrial membrane, which is the rate-limiting step in neurosteroid biosynthesis. Neurosteroids interact with non benzodiazepine site of GABAa receptor causing an anxiolytic effect without the side effects.

Methods: Using the original peptide drug-based design strategy, the first putative dipeptide ligand of the TSPO N-carbobenzoxy-L-tryptophanyl-L-isoleucine amide (GD-23) was obtained. Read More

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http://dx.doi.org/10.2174/1573406415666181119164846DOI Listing
November 2018
7 Reads

Spirocyclohexadienones as an Uncommon Scaffold for Acetylcholinesterase Inhibitory Activity.

Med Chem 2018 Nov 8. Epub 2018 Nov 8.

Laboratório de Síntese de Produtos Naturais e Fármacos - Institute of Chemistry, University of Campinas, PO Box 6154 - 13083-970 - Campinas, SP . Brazil.

The potential of inhibition of a set of some spirocyclohexadienones, readily synthesized in two steps and good overall yield from Morita-Baylis-Hillman adducts, was evaluated in vitro against acetylcholinesterase. We found that eight of them are able to inhibit the acetylcholinesterase activity, with IC50 values ranging from 0.12 to 12. Read More

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http://dx.doi.org/10.2174/1573406414666181109114214DOI Listing
November 2018
8 Reads

Synthesis, Anti-varicella-zoster virus and Anti-cytomegalovirus Activity of 4,5-Disubstituted 1,2,3-(1H)-Triazoles.

Med Chem 2018 Nov 8. Epub 2018 Nov 8.

School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 100081. China.

Background: Clinical drugs for herpesvirus exhibit high toxicity and suffer from significant drug-resistantance. The development of new, effective, and safe anti-herpesvirus agents with different mechanisms of action is greatly required.

Objective: Novel inhibitors against herpesvirus with different mechanisms of action from that of clinical drugs. Read More

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http://dx.doi.org/10.2174/1573406414666181109095239DOI Listing
November 2018
10 Reads

Design, synthesis, antimicrobial and anti-biofilm evaluation, and molecular docking of new substituted fluoroquinazolinones.

Med Chem 2018 Nov 8. Epub 2018 Nov 8.

Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Al-Madinah Al-Munawarah. Saudi Arabia.

Background: Quinazolines and quinazolinones derivatives are well known for their important range of therapeutic activities.

Objective: Synthesis of some derivatives of substituted fluoroquinazolinones based on structure-based design and evaluation of their antibacterial, antifungal, and anti-biofilm activities.

Method: Compounds were chemically synthesized by conventional methods. Read More

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http://www.eurekaselect.com/167188/article
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http://dx.doi.org/10.2174/1573406414666181109092944DOI Listing
November 2018
11 Reads

Pyrrolopyrazoles; Synthesis, Evaluation and Pharmacological Screening as Antidepressant Agents.

Med Chem 2018 Nov 7. Epub 2018 Nov 7.

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Ain-Helwan, Postal code:11795, Helwan, Cairo. Egypt.

• Background: Pyrroles and fused pyrroles are of great interest as biologically active compounds, among these activities; antidepressant activity is of special concern.

Objective: Synthesis of a series of pyrrolopyrazoles and their pyrimidine derivatives and their characterization using spectral data to be monitored for antidepressant activity using behavioral techniques.

Method: A control group provided by the vehicle i. Read More

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http://www.eurekaselect.com/167163/article
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http://dx.doi.org/10.2174/1573406414666181108090321DOI Listing
November 2018
7 Reads

Synthesis and biological evaluation of polyfluoroalkylated antipyrines and their isomeric O-methylpyrazoles.

Med Chem 2018 Nov 6. Epub 2018 Nov 6.

Ufa Institute of Chemistry of Russian Academy of Science, Octyabrya Av., 71, Ufa 450078. Russian Federation.

Background: Formally belonging to the non-steroidal anti-inflammatory drug class pyrazolones have long been used in medical practices.

Objective: Our goal is to synthesize N-methylated 1-aryl-3-polyfluoroalkylpyrazolones as fluorinated analogs of antipyrine, their isomeric O-methylated derivatives resembling celecoxib structure and evaluate biological activities of obtained compounds.

Methods: In vitro (permeability) and in vivo (anti-inflammatory and analgesic activities, acute toxicity, hyperalgesia, antipyretic activity, "open field" test) experiments. Read More

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http://dx.doi.org/10.2174/1573406414666181106145435DOI Listing
November 2018
1 Read

Small Molecular Leads Differentially Active against HER2 Positive and Triple Negative Breast Cancer Cell Lines.

Med Chem 2018 Nov 6. Epub 2018 Nov 6.

Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270. Pakistan.

Background: Breast cancer is the most prevalent cancer type in women globally. It is characterized by distinct subtypes depending on different gene expression pattern. Oncogene HER2 is expressed on the surface of cell, and is responsible for cell growth regulation. Read More

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http://dx.doi.org/10.2174/1573406414666181106143912DOI Listing
November 2018
8 Reads

Design, synthesis and in vitro evaluation of novel anti-HIV 3-pyrazol-3-yl-pyridin-2-one analogs.

Med Chem 2018 Nov 6. Epub 2018 Nov 6.

Department of Natural Products, National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S. A. S. Nagar-160 062, Punjab. India.

Background: Natural products have shown potent anti-HIV activity, but some of these also possess toxicity. The pharmacophoric fragments of these natural products have scope of combination with other pharmacophoric fragment and derivatization to reduce toxicity and increase the potency. Combination of natural product fragments from different classes of anti-HIV compounds may lead to a new class of potent anti-HIV agents. Read More

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http://dx.doi.org/10.2174/1573406414666181106125539DOI Listing
November 2018
18 Reads

Design and synthesis novel sulfonamide-derived triazoles and bioactivity exploration.

Med Chem 2018 Nov 6. Epub 2018 Nov 6.

School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715. China.

Objective: Due to incidence of resistance, a series of sulfonamide-derived 1,2,4-triazoles were synthesized and evaluated.

Results: In vitro antimicrobial evaluation found that 2-chlorobenzyl sulfonamide 1,2,4-triazole 7c exhibited excellent antibacterial activities against MRSA, B. subtilis, B. Read More

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http://dx.doi.org/10.2174/1573406414666181106124852DOI Listing
November 2018
11 Reads

Synthesis and Evaluation of Antifungal and Antitrypanosomastid Activities of Symmetrical 1,4-Disubstituted-1,2,3-Bistriazoles Obtained by CuAAC Conditions.

Med Chem 2018 10 24. Epub 2018 Oct 24.

Biomedical Sciences Institute, Federal University of Alfenas, Alfenas 37130-000, MG. Brazil.

Background: The trypanosomatids, such as the protozoan Leishmania spp., have a demand by ergosterol, which is not present in the membrane from mammal cells. The suppression of the synthesis of ergosterol would be a new target of compounds with leishmanicidal activity, and bistriazole has showed trypanocidal activity by this mechanism. Read More

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http://dx.doi.org/10.2174/1573406414666181024111522DOI Listing
October 2018

Synthesis of new thiosemicarbazones and semicarbazones containing the 1,2,3-1H-triazole-isatin scaffold: trypanocidal, cytotoxicity, electrochemical assays, and molecular docking.

Med Chem 2018 Sep 12. Epub 2018 Sep 12.

Instituto de Quimica (IQ), Universidade Federal do Rio de Janeiro (UFRJ), Av. Athos da Silveira Ramos, 149, Cidade Universitária, Ilha do Fundão, 21949-900, Rio de Janeiro, RJ. Brazil.

Background: Chagas disease, also known as American trypanosomiasis, is classified as one of the 17 most important neglected diseases by the World Health Organization. The only drugs with proven efficacy against Chagas disease are benznidazole and nifurtimox, however both show adverse effects, poor clinical efficacy,and the development of resistance. For these reasons, the search for new effective chemical entities is a challenge to research groups and the pharmaceutical industry. Read More

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http://www.eurekaselect.com/165353/article
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http://dx.doi.org/10.2174/1573406414666180912120502DOI Listing
September 2018
4 Reads

Novel Guanosine Derivatives as Anti-HCV NS5b polymerase: A QSAR and Molecular Docking Study.

Authors:
Abdo A Elfiky

Med Chem 2018 Oct 15. Epub 2018 Oct 15.

Biophysics Department, Faculty of Science, Cairo University, Giza. Egypt.

Background: IDX-184 is a guanosine derivative having a potent inhibitory performance against HCV NS5b polymerase.

Objective: to test three different groups of 2'C - modified analogues of guanosine nucleotide against HCV polymerase.

Method: Using combined Quantitative Structure-Activity Relationships (QSAR) and molecular docking, the suggested compounds are studied. Read More

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http://www.eurekaselect.com/166272/article
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http://dx.doi.org/10.2174/1573406414666181015152511DOI Listing
October 2018
5 Reads

Design, synthesis and anticancer evaluation of novel series of Indibulin analogues.

Med Chem 2018 Oct 15. Epub 2018 Oct 15.

Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran 1417614411. Iran.

Background: cancer is an important cause of human death worldwide. During last decades many anticancer agents with anti-tubulin mechanism have been synthesized or extracted from nature and some of them also entered to clinical use. Indibulin is one of the most potent tubulin polymerization inhibitor with minimal peripheral neuropathy which is a big problem by some of antimitotic agents such as taxanes and vinka alkaloids. Read More

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http://dx.doi.org/10.2174/1573406414666181015145945DOI Listing
October 2018
19 Reads

Synthesis and Biological Evaluation of Acridine/Acridone Analogs as Potential Anticancer Agents.

Med Chem 2018 Oct 15. Epub 2018 Oct 15.

Department of Organic Chemistry, Gdansk University of Technology, Narutowicza St 11/12, PL 80-233 Gdansk. Poland.

Background: The lack of efficacious therapy for advanced melanoma and neuroblastoma makes new approaches necessary. Therefore, many scientists seek new, more effective, more selective and less toxic anticancer drugs.

Objective: We propose the synthesis of the new functionalized analogs of 1-nitroacridine/4-nitroacridone connected to tuftsin/retro-tuftsin derivatives as potential anticancer agents. Read More

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http://www.eurekaselect.com/166258/article
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http://dx.doi.org/10.2174/1573406414666181015145120DOI Listing
October 2018
10 Reads

Evaluation of antiplasmodial potential of C-2 and C-8 modified quinolines: in vitro and in silico study.

Med Chem 2018 Oct 15. Epub 2018 Oct 15.

Natural Product Chemistry and Process Development Division, CSIR-Institute of Himalayan Bioresource Technology, Palampur, Himachal Pradesh 176 061. India.

Background: Malaria remains a common life-threatening infectious disease across the globe due to the development of resistance by Plasmodium parasite against most antimalarial drugs. The situation demands new and effective drug candidates against Plasmodium.

Objectives: The objective of this study is to design, synthesize and test novel quinoline based molecules against the malaria parasite. Read More

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http://dx.doi.org/10.2174/1573406414666181015144413DOI Listing
October 2018
4 Reads
1.390 Impact Factor

Synthesis and biological evaluation of scutellarein alkyl derivatives as preventing neurodegenerative agents with improved lipid soluble properties.

Med Chem 2018 Oct 15. Epub 2018 Oct 15.

Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization, Jiangsu Key Laboratory for High Technology Research of TCM Formulae, National and Local Collaborative Engineering Center of Chinese Medicinal Resources Industrialization and Formulae Innovative Medicine, Nanjing University of Chinese Medicine, Nanjing, Jiangsu. China.

Background: Exogenous antioxidants are considered as a promising therapeutic approach to treat neurodegenerative diseases, since they could prevent and/or minimize the neuronal damage by oxidation.

Objective: Three series of lipophilic compounds structurally based on scutellarein (2), which is one metabolite of scutellarin (1) in vivo, have been designed and synthesized.

Method: Their antioxidant activity was evaluated by detecting the 2-thiobarbituric acid reactive substance (TBARS) produced in the ferrous salt/ascorbate induced autoxidation of lipids, which were present in microsomal membranes of rat hepatocytes. Read More

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http://dx.doi.org/10.2174/1573406414666181015143551DOI Listing
October 2018

Novel conjugated unsaturated ketones with submicromolar potencies towards some leukemic and colon cancer cells.

Med Chem 2018 Oct 15. Epub 2018 Oct 15.

Drug Discovery and Development Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, 104 Clinic Place, Saskatoon, Saskatchewan S7N 2Z5. Canada.

Background: Cancer continues to be the major health burden worldwide. There is an urgent need for the development of novel antineoplastic compounds to treat this devastating condition. Various alkylating anticancer drugs have been employed in the clinic for treating cancers. Read More

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http://www.eurekaselect.com/166245/article
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http://dx.doi.org/10.2174/1573406414666181015142633DOI Listing
October 2018
9 Reads

Antiprotozoal Activities of Tetrazole-quinolines with Aminopiperidine Linker.

Med Chem 2018 Oct 15. Epub 2018 Oct 15.

Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, University of Graz. Australia.

Background: Human African Trypanosomiasis (HAT, sleeping sickness) and Malaria both are insect vectored tropical diseases. Only a couple of drugs is able to cure HAT, but all of them are toxic, prone to resistance and require parenteral administration. Malaria is responsible for high morbidity and mortality in humans. Read More

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http://www.eurekaselect.com/166231/article
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http://dx.doi.org/10.2174/1573406414666181015115101DOI Listing
October 2018
7 Reads

Carbonic anhydrase inhibitory potential of 1,2,4-triazole-3-thione derivatives of flurbiprofen, ibuprofen and 4-tert-butylbenzoic hydrazide : Design, synthesis, characterization, biochemical evaluation, molecular docking and dynamic simulation studies.

Med Chem 2018 Oct 12. Epub 2018 Oct 12.

Centre for Advanced Drug Research, COMSATS University Islamabad, Abbottabad Campus, Abbottabad-22060. Pakistan.

Background: The over-expression of the carbonic anhydrases results in some specific carcinomas including pancreatic, gastric and brain tumor. Tumors are distinguished under hypoxic conditions and various investigations are being carried out to target the known hypoxic areas of the tumors to increase the sensitivity towards standard therapeutic treatment.

Objective: Herein, we have designed and synthesized some biologically important esters, hydrazides, thiocarbamates, 1,2,4-triazole-3-thiones and Schiff bases. Read More

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http://www.eurekaselect.com/166217/article
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http://dx.doi.org/10.2174/1573406414666181012165156DOI Listing
October 2018
5 Reads