1,606 results match your criteria Medicinal Chemistry[Journal]


Synthesis of β-Ketosulfone Derivatives As New Non-Cytotoxic Urease Inhibitors In Vitro.

Med Chem 2019 Apr 15. Epub 2019 Apr 15.

H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270. Pakistan.

Background: Peptic ulcer and urolithiasis are largely due to infection caused by urease producing bacteria. Therefore, discovery of urease inhibitors is an important area of medicinal chemistry research.

Objective: The main goal of the work was to identify novel urease inhibitors with no cytotoxicity. Read More

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http://dx.doi.org/10.2174/1573406415666190415163309DOI Listing
April 2019
4 Reads

Synthesis and biological evaluation of 5-benzyl-3-pyridyl-1H-1,2,4-triazole derivatives as xanthine oxidase inhibitors.

Med Chem 2019 Apr 9. Epub 2019 Apr 9.

School of Pharmacy, China Medical University, 77 Puhe Road, North New Area, Shenyang 110122. China.

Background: Topiroxostat is an excellent xanthine oxidase (XO) inhibitor, possessing a specific 3,5-diaryl-1,2,4-triazole framework.

Objective: The present work was aimed to investigate the preliminary structure-activity relationship (SAR) of 2-cyanopyridine-4-yl-like fragments of topiroxostat analogues.

Methods: A series of 5-benzyl-3-pyridyl-1H-1,2,4-triazole derivatives (1a-j and 2a-j) was designed and synthesized by replacement of the 2-cyanopyridine-4-yl moiety with substituted benzyl groups. Read More

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http://www.eurekaselect.com/171471/article
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http://dx.doi.org/10.2174/1573406415666190409112209DOI Listing
April 2019
3 Reads
1.387 Impact Factor

Novel Coupled Molecules from Active Structural Motifs of Synthetic and Natural Origin as Immunosuppressants.

Med Chem 2019 Apr 9. Epub 2019 Apr 9.

Department of Pharmaceutical Sciences and Drug Research Punjabi University, Patiala. India.

Introduction: Nitric oxide (NO) is an important mediator in pathogenesis and control of immune system-related disorders and its levels are modulated by inducible NO synthase (iNOS). Oxidative stress is another pathological indication in majority of autoimmune disorders. The present study aims at development of coupled molecules via selection of pharmacophores for both immunomodulatory through iNOS inhibition and antioxidant activities. Read More

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http://dx.doi.org/10.2174/1573406415666190409111459DOI Listing
April 2019
2 Reads

Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents.

Med Chem 2019 Apr 8. Epub 2019 Apr 8.

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562. Egypt.

Background: Marine sponges and tunicates have been a wealthy source of cytotoxic compounds such as indole alkaloids. Most of the indole alkaloids showed in vitro cytotoxic and anti-neoplastic activities against wide range of cancer cell lines.

Objective: Three series of bioisosteres of marine indole alkaloids (meridianins) were synthesized and the compounds were tested for their in vitro anti-proliferative activity against HCT-116 cell-line. Read More

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http://www.eurekaselect.com/171419/article
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http://dx.doi.org/10.2174/1573406415666190408125514DOI Listing
April 2019
1 Read

First example of antiparasitic activity influenced by thermochromism: Leishmanicidal evaluation of 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine metal complexes.

Med Chem 2019 Apr 1. Epub 2019 Apr 1.

Department of Parasitology, Faculty of Sciences, University of Granada Avda. Fuentenueva, 18071 Granada. Spain.

Background: The World Health Organization catalogues illnesses such as Leishmaniasis as neglected diseases, due to the low investment in new drugs to fight them. The search of novel and non-side effects anti-parasitic compounds is one of the urgent needs for the Third World. The use of triazolopyrimidines and their metallic complexes have demonstrated hopeful results in this field. Read More

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http://dx.doi.org/10.2174/1573406415666190401120607DOI Listing
April 2019
1 Read

Design and Synthesis of New Sulfonamides-Based Flt3 Inhibitors.

Med Chem 2019 Apr 1. Epub 2019 Apr 1.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Jordan, Amman. Jordan.

Background: Flt3 is an oncogenic kinase involved in different leukemias. It is most prominently associated with acute myeloid leukemia (AML). Flt3-specific inhibitors have shown promising results in interfering with AML. Read More

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http://dx.doi.org/10.2174/1573406415666190401144053DOI Listing
April 2019
4 Reads

Novel amide derivatives as potent tyrosinase inhibitors; in-vitro, in-vivo antimelanogenic activity and computational studies.

Med Chem 2019 03 18. Epub 2019 Mar 18.

Plasma Bioscience Research Center, Kwangwoon University, 20 Kwangwoon-gil, Nowon-gu, Seoul 139-701. Korea.

Background: Tyrosinase is involved in melanin biosynthesis and the abnormal accumulation of melanin pigments leading to hyperpigmentation disorders. Controlling the melanogenesis could be an important strategy for treating abnormal pigmentation.

Methods: In present study a series of amide derivatives (3a-e and 5a-e) were synthesized aiming to inhibit tyrosinase activity and melanin production. Read More

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http://dx.doi.org/10.2174/1573406415666190319101329DOI Listing
March 2019
4 Reads

Preface.

Prog Med Chem 2019 ;58:ix-x

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http://dx.doi.org/10.1016/S0079-6468(19)30009-8DOI Listing
January 2019

Amyotrophic lateral sclerosis.

Prog Med Chem 2019 8;58:63-117. Epub 2019 Mar 8.

Department of Biological Sciences, The University of Alabama, Tuscaloosa, AL, United States.

Amyotrophic lateral sclerosis (ALS) is caused by selective and progressive loss of spinal, bulbar and cortical motoneurons and leads to irreversible paralysis, loss of speech, inability to swallow and respiratory malfunctions with the eventual death of the affected individual in a rapid disease course. Several suggested molecular pathways are reviewed including SOD1 gene mutation, protein nitrosylation, phosphorylation and oxidative stress, excitotoxicity, glutamate transporter deprivation, mitochondrial involvement, protein aggregation and motor neuron trophic factors. The role of insulin and its receptor in the brain is described. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S00796468183001
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http://dx.doi.org/10.1016/bs.pmch.2018.12.001DOI Listing
March 2019
7 Reads

Natural product drug delivery: A special challenge?

Prog Med Chem 2019 1;58:157-187. Epub 2019 Mar 1.

Novartis Institutes for Biomedical Research, Basel, Switzerland.

Natural products have a long-standing and critical role in drug development and medical use. The structural and physicochemical properties of natural products, while derived evolutionarily to be effective in living systems, may create challenges in translation to a pharmaceutical product. Molecular complexity, low solubility, functional group reactivity and general instability are among the challenges that typically need to be overcome. Read More

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http://dx.doi.org/10.1016/bs.pmch.2019.01.001DOI Listing
March 2019
1 Read

Rewriting the (tran)script: Application to spinal muscular atrophy.

Prog Med Chem 2019 1;58:119-156. Epub 2019 Feb 1.

F. Hoffmann-La Roche Ltd., pRED, Pharma Research & Early Development, Roche Innovation Center Basel, Basel, Switzerland.

Targeting RNA drastically expands our target space to therapeutically modulate numerous cellular processes implicated in human diseases. Of particular interest, drugging pre-mRNA splicing appears a very viable strategy; to control levels of splicing product by promoting the inclusion or exclusion of exons. After describing the concept of "splicing modulation", this chapter will cover the outstanding progress achieved in this field, by highlighting the breakthrough accomplished recently for the treatment of spinal muscular atrophy using two therapeutic modalities: splice switching oligonucleotides and small molecules. Read More

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http://dx.doi.org/10.1016/bs.pmch.2018.12.003DOI Listing

Covalent binders in drug discovery.

Prog Med Chem 2019 11;58:1-62. Epub 2019 Mar 11.

AbbVie Inc., North Chicago, IL, United States.

Covalent modulation of protein function can have multiple utilities including therapeutics, and probes to interrogate biology. While this field is still viewed with scepticism due to the potential for (idiosyncratic) toxicities, significant strides have been made in terms of understanding how to tune electrophilicity to selectively target specific residues. Progress has also been made in harnessing the potential of covalent binders to uncover novel biology and to provide an enhanced utility as payloads for Antibody Drug Conjugates. Read More

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http://dx.doi.org/10.1016/bs.pmch.2018.12.002DOI Listing

Synthesis, biological evaluation and molecular dynamics simulation studies of novel diphenyl ethers.

Med Chem 2019 Mar 6. Epub 2019 Mar 6.

Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal-576104. India.

A series of novel N-(1-(3-hydroxy-4-phenoxyphenyl)-3-oxo-3-phenylpropyl)acetamides and N-(3(3-hydroxy-4phenoxyphenyl)-3-oxo-1-phenylpropyl) acetamides were designed, synthesized, and evaluated against HepG2, A-549, MCF-7 and Vero cell lines. Among the tested compounds, compound 3d was most active (IC50 13.76 ± 0. Read More

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http://dx.doi.org/10.2174/1573406415666190306152907DOI Listing

Bicycloheptylamine-Doxorubicin Conjugate: Synthesis and Anticancer Activities in σ2 Receptor-Expressing Cell Lines.

Med Chem 2019 Mar 1. Epub 2019 Mar 1.

Department of Pharmaceutical Sciences, Philadelphia College of Pharmacy, University of the Sciences in Philadelphia, Philadelphia. United States.

Background: Novel bicycloheptylamines were designed and synthesized. These compounds were found to be selective for sigma-2 receptors. These receptors have been found to be up to 10 fold over-expressed in certain cancer cell lines, leading to investigation of possible uses as a biomarker in diagnosis and/or treatment especially in cancers with poor prognosis. Read More

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http://dx.doi.org/10.2174/1573406415666190301145203DOI Listing
March 2019
1 Read

Design, Synthesis, and Biological Evaluation of Novel C5-Modified Pyrimidine Ribofuranonucleosides as Potential Antitumor or/and Antiviral Agents.

Med Chem 2019 Feb 24. Epub 2019 Feb 24.

Department of Biochemistry and Biotechnology, Laboratory of Bioorganic Chemistry, University of Thessaly, Larissa. Greece.

Background: Nucleoside analogues are well known antitumor, antiviral, and chemotherapeutic agents. Alterations on both their sugar and the heterocyclic parts may lead to significant changes in the spectrum of their biological action and the degree of selective toxicity, as well as in their physicochemical properties.

Method: C5-arylalkynyl-β-D-ribofuranonucleosides 3-6, 3΄-deoxy 12-15, 3΄-deoxy-3΄-C-methyl-β-D-ribofurananucleosides 18-21 and 2΄-deoxy-β-D-ribofuranonucleosides 23-26 of uracil, were synthesized using a one-step Sonogashira reaction under microwave irradiation and subsequent deprotection. Read More

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http://dx.doi.org/10.2174/1573406415666190225112950DOI Listing
February 2019
1 Read

Design and synthesis of new substituted pyrazolopyridines with potent antiproliferative activity.

Med Chem 2019 Feb 22. Epub 2019 Feb 22.

Department of Nutrition & Dietetics, School of Health Sciences and Education, Harokopio University, Athens 17671. Greece.

Background: Purine isosteres are often endowed with interesting pharmacological properties, due to their involvement in cellular processes replacing the natural purines. Among these compounds, pyrazolopyridines are under active investigation for potential anticancer properties.

Objectives: Based on previously discovered substituted pyrazolopyridines with promising antiproliferative activity, we designed and synthesized new, suitably substituted analogues aiming to investigate their potential activity and contribute to SAR studies of this class of bioactive compounds. Read More

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http://dx.doi.org/10.2174/1573406415666190222130225DOI Listing
February 2019
5 Reads

Discovery and optimization of a series of sulfonamide inverse agonists for the retinoic acid receptor-related receptor-α.

Med Chem 2019 Feb 22. Epub 2019 Feb 22.

Molecular Medicine, The Scripps Research Institute, Jupiter, Florida 33458. United States.

Background: Despite a massive industry endeavor to develop RORy-modulators for autoimmune disorders, there has been no indication of efforts to target the close family member RORα for similar indications. This may be due to the misconception that RORα is redundant to RORy, or the inherent difficulty in cultivating tractable starting points for RORα. RORα-selective modulators would be useful tools to interrogate the biology of this understudied orphan nuclear receptor. Read More

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http://dx.doi.org/10.2174/1573406415666190222124745DOI Listing
February 2019
4 Reads
1.387 Impact Factor

Discovery of new Phosphoinositide 3-kinase delta (PI3Kδ) inhibitors via virtual screening using crystallography-derived pharmacophore modelling and QSAR analysis.

Med Chem 2019 Feb 22. Epub 2019 Feb 22.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman. Jordan.

Background: PI3Kδ is predominantly expressed in hematopoietic cells and participates in the activation of leukocytes. PI3Kδ inhibition is promising approach for treating inflammatory diseases and leukocyte malignancies. Accordingly, we decided to model PI3Kδ binding. Read More

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http://dx.doi.org/10.2174/1573406415666190222125333DOI Listing
February 2019
1 Read

New Copper Compounds with Antiplatelet Aggregation Activity.

Med Chem 2019 Feb 22. Epub 2019 Feb 22.

Instituto Nacional de Cardiología Ignacio Chavez. Juan Badiano 1, Tlalpan 14080, Ciudad de Mexico. Mexico.

Background: Ischemic heart disease, cerebrovascular accident, and venous thromboembolism have the presence of a thrombotic event in common and represent the most common causes of death within the population.

Objective: Since Schiff base copper(II) complexes are able to interact with polyphosphates (PolyP), a procoagulant and potentially prothrombotic platelet agent, we investigated the antiplatelet aggregating properties of two novel tridentate Schiff base ligands and their corresponding copper(II) complexes.

Methods: The Schiff base ligands (L1) and (L2), as well as their corresponding copper(II) complexes (C1) and (C2), were synthesized and characterized by chemical analysis, X-ray diffraction, mass spectrometry, and UV-Visible, IR and far IR spectroscopy. Read More

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http://dx.doi.org/10.2174/1573406415666190222123207DOI Listing
February 2019
1 Read
1.387 Impact Factor

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
2 Reads

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
1 Read

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
2 Reads

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
1.387 Impact Factor

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
1.387 Impact Factor

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://www.eurekaselect.com/169726/article
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http://dx.doi.org/10.2174/1573406415666190206231002DOI Listing
February 2019
3 Reads

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
1 Read

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
1 Read

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
1 Read

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
2 Reads

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
5 Reads

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
13 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
3 Reads

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
1 Read

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
14 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
24 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
8 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
4 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
4 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
2 Reads

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
1 Read

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
9 Reads