502 results match your criteria Current Drug Discovery Technologies[Journal]


Using PBPK Modeling to Predict Drug Exposure and Support Dosage Adjustments in Patients With Renal Impairment: An Example With Lamivudine.

Curr Drug Discov Technol 2019 Feb 14. Epub 2019 Feb 14.

Samuel J. and Joan B. Williamson Institute for Pharmacometrics, Division of Pharmaceutical Sciences, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, New York. United States.

Background: Lamivudine is a nucleoside reverse transcriptase inhibitor used to treat HIV and hepatitis B. It is primarily cleared by the kidney with renal secretion mediated by OCT2 and MATE.

Objective: To use PBPK modeling to assess the impact of renal impairment on lamivudine pharmacokinetics using the Simcyp® Simulator. Read More

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http://dx.doi.org/10.2174/1570163816666190214164916DOI Listing
February 2019

In silico Inhibition of BACE-1 by Selective Phytochemicals as Novel Potential Inhibitors: Molecular Docking and DFT Studies.

Curr Drug Discov Technol 2019 Feb 14. Epub 2019 Feb 14.

Department of Life Sciences, University of Management and Technology, Lahore. Pakistan.

Background: Alzheimer's disease (AD) has become the most common age-dependent disease of dementia. The trademark pathologies of AD are the presence of amyloid aggregates in neurofibrils. Recently phytochemicals being considered as potential inhibitors against various neurodegenerative, anti-fungal, antibacterial and antiviral diseases in human beings. Read More

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http://dx.doi.org/10.2174/1570163816666190214161825DOI Listing
February 2019

In vitro protective effect of ascorbic acid against antibiotic-induced hepatotoxicity.

Curr Drug Discov Technol 2019 Feb 4. Epub 2019 Feb 4.

Dept. of Pharmacology, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Science Campus, Kochi, Kerala. India.

Background: Although antibiotic-induced hepatotoxicity is recoverable with mild impairment, and few of them were reported to cause morbidity. Hence, an adjuvant is essential in reducing such incidences.

Objective: The aim of this study to evaluate the protective effect of ascorbic acid on antibiotic induced liver toxicity using liver slices. Read More

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http://dx.doi.org/10.2174/1570163816666190204122007DOI Listing
February 2019
4 Reads

Antimicrobial Activity of Agarwood Oil against Multiple-Drug-Resistant (MDR) Microbes of Clinical, Food and Environmental Origin.

Curr Drug Discov Technol 2019 Jan 25. Epub 2019 Jan 25.

Division of Medicine, ICAR-Indian Veterinary Research Institute, Izatnagar-243 122. India.

Background And Objectives: Multiple-Drug-Resistance (MDR) among bacteria is imminent problem and alternative therapies are seen as future abode. Agarwood Oil (AO) is described to possess antimicrobial activity besides many other medicinal utilities. This paper discusses antimicrobial activity of AO on MDR and non-MDR strains of microbes of 69 genera isolated from clinical and non-clinical samples. Read More

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http://dx.doi.org/10.2174/1570163816666190125163536DOI Listing
January 2019

The Role of Anthocyanins in Drug Discovery: Recent Developments.

Curr Drug Discov Technol 2019 Jan 25. Epub 2019 Jan 25.

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Rende (CS). Italy.

Natural compounds have always played a key role in drug discovery. Anthocyanins are secondary metabolites belonging to the flavonoids family responsible for the purple, blue, and red colour of many vegetables and fruits. These phytochemicals have attracted the interest of researchers for their important implications in human health and for their use as natural colorants. Read More

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http://dx.doi.org/10.2174/1570163816666190125152931DOI Listing
January 2019

Therapeutic aspects of Squill; an evidence-based review.

Curr Drug Discov Technol 2019 Jan 25. Epub 2019 Jan 25.

Department of Persian Medicine, School of Persian and Complementary Medicine, Mashhad University of Medical Sciences, Mashhad. Iran.

From ancient times, medicinal plants have been usually utilized to treat many disorders, but today, interest in these herbs is again aroused, because of their fewer side effects and low-cost. In traditional medicine, for many diseases, various medicinal herbs have been suggested so far. Drimia maritime, also named squill, is an important medicinal plant for the treatment of many diseases, especially respiratory diseases. Read More

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http://dx.doi.org/10.2174/1570163816666190125154745DOI Listing
January 2019
1 Read

Cinnamaldehyde Analogs: Docking Based Optimization, COX-2 Inhibitory in vivo and in vitro Studies.

Curr Drug Discov Technol 2019 Jan 25. Epub 2019 Jan 25.

Department of Pharmacy, Lala Lajpat Rai Memorial Medical College, Meerut, Uttar Pradesh. India.

The research work aims to investigate Schiff bases of Cinnamaldehyde as biologically potent analogs. In the past decade CADD has emerged as a rational approach in drug development so with the help molecular docking approach we planned to perform virtual screening of the designed data set of Schiff bases. This will be helpful to put some light on the drug receptor interactions required for anti-inflammatory activity. Read More

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http://dx.doi.org/10.2174/1570163816666190125153951DOI Listing
January 2019

An herbal H2 blocker in melasma treatment.

Curr Drug Discov Technol 2019 Jan 21. Epub 2019 Jan 21.

Health center, Mashhad University of Medical Sciences, Mashhad. Iran.

Background: Melasma is a skin pigmentation disorder that remains resistant to available therapies. The exact cause of melasma is unknown. Histamine is an inflammatory factor. Read More

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http://dx.doi.org/10.2174/1570163816666190121145653DOI Listing
January 2019

From Target identification to Drug Development in Space: Using the Microgravity Assist.

Authors:
Martin Braddock

Curr Drug Discov Technol 2019 Jan 12. Epub 2019 Jan 12.

Sherwood Observatory, Mansfield and Sutton Astronomical Society, Coxmoor Road, Sutton-in-Ashfield, Nottinghamshire,. United Kingdom.

The unique nature of microgravity encountered in space provides an opportunity for drug discovery and development that cannot be replicated on Earth. From the production of superior protein crystals to the identification and validation of new drug targets to microarray analyses of transcripts attenuated by microgravity, there are numerous examples which demonstrate the benefit of exploiting the space environment. Moreover, studies conducted on Space Shuttle missions, the International Space Station and other craft have had direct benefit for drug development programmes such as those directed against reducing bone and muscle loss or increasing bone formation. Read More

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http://dx.doi.org/10.2174/1570163816666190112150014DOI Listing
January 2019
1 Read

Novel approaches to anti-atherosclerotic therapy: Cell-based models and herbal preparations (Review of our own data).

Curr Drug Discov Technol 2018 Dec 31. Epub 2018 Dec 31.

Department of Neurochemistry, Division of Basic and Applied Neurobiology, Serbsky Federal Medical Research Center of Psychiatry and Narcology, 119991 Moscow. Russian Federation.

Atherosclerosis is a chronic arterial disease characterized by vascular inflammation, accumulation of lipids in the arterial wall, and formation and growth of atherosclerotic plaques followed by ischemia. In subclinical atherosclerosis, cholesterol retention in subendothelial cells leads to induction of local inflammation, generation of foam cells and lesion formation, followed by a chain of other pathogenic events. Atherosclerotic progression can frequently be fatal, since plaque rupture may lead to thrombosis and acute events, such as myocardial infarction, stroke and sudden death. Read More

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http://dx.doi.org/10.2174/1570163816666190101112241DOI Listing
December 2018
5 Reads

Structure-Activity Relationships of Cytotoxic Lactones as Inhibitors and Mechanisms of Action.

Curr Drug Discov Technol 2018 Dec 31. Epub 2018 Dec 31.

Departamento de Ciencias Experimentales y Matemáticas, Facultad de Veterinaria y Ciencias Experimentales, Universidad Católica de Valencia San Vicente Mártir, Guillem de Castro-94, E 46001 Valè ncia. Spain.

Background: Some lactones prevent protein Myb-dependent gene expression.

Objective: The object is to calculate inhibitors of Myb-brought genetic manifestation.

Method: Linear quantitative structure-potency relations result expanded, among sesquiterpene lactones of a huge macrocycle variety (pseudoguaianolides, guaianolides, eudesmanolides and germacranolides), to establish which part of the molecules constitutes their pharmacophore, and predict their inhibitory potency on Myb-reliant genetic manifestation, which may result helpful as leads for antileukaemia therapies with a new mechanism of action. Read More

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http://dx.doi.org/10.2174/1570163816666190101113434DOI Listing
December 2018
3 Reads

PCSK9 inhibitors and cardiovascular disease: impact on cardiovascular outcomes.

Curr Drug Discov Technol 2018 12 10. Epub 2018 Dec 10.

Department of Endocrinology, Diabetes and Metabolism, Evangelismos Hospital, Athens. Greece.

Cardiovascular disease (CAD) remains the leading cause of morbidity and mortality in the western world. Hypolipidemic drugs have long been used for the primary and secondary prevention of heart disease. However, the high frequency of recurrent events in patients despite on hypolipidemic therapy has increased the need for new more targeted therapeutic approaches. Read More

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http://www.eurekaselect.com/168232/article
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http://dx.doi.org/10.2174/1570163816666181211112358DOI Listing
December 2018
4 Reads

Efficacy of β-D-mannuronic acid [M2000] on pro-apoptotic process and inflammatory related molecules NFҡB, IL-8 and Cd49d using healthy donor PBMC.

Curr Drug Discov Technol 2018 Nov 9. Epub 2018 Nov 9.

Department of Immunology, School of Public Health, Tehran University of Medical Sciences, Tehran. Iran.

This investigation evaluates the pro-apoptotic and anti-inflammatory effects of β-D-mannuronic acid [M2000] compared to diclofenac, based on gene expression involved in apoptosis and inflammation process [including Bcl2, NFκB, IL-8 and Cd49d] in peripheral blood mononuclear cells [PBMCs] of healthy donors under exvivo conditions. The venous blood of twelve healthy volunteers with aged 25-60 years, were collected in heparinized tubes. The healthy volunteers were selected from no smoking group and without using illicit drugs and suffering from diabetes. Read More

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http://dx.doi.org/10.2174/1570163815666181109165837DOI Listing
November 2018
3 Reads

Design, Synthesis and Pharmacological evalution of 1,3,4-Oxadiazole Derivatives As Collapsin Response Mediator Protein 1 (CRMP 1) Inhibitors.

Curr Drug Discov Technol 2018 Nov 5. Epub 2018 Nov 5.

Department of Pharmaceutical chemistry, Parul institute of pharmacy, Parul University, Vadodara-391760, Gujarat. India.

Context: objective: The series of 2-(4-Phenylamino)-N-(5-((4-nitrophenoxy)methyl) -1,3,4-oxadiazol-2-yl)acetamide (5a-5e) and substituted N-(5-(Phenoxymethyl)-1,3,4-oxadiazol-2-yl)-2-(phenylamino)acetamide (5f-5i) were designed, synthesized and investigated for Collapsin response mediator protein 1 (CRMP 1) inhibitors as small lung cancer.

Design: Design of compounds was done by literature review and molecular docking studies in iGEMDOCK 2.0. Read More

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http://www.eurekaselect.com/167058/article
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http://dx.doi.org/10.2174/1570163815666181106090708DOI Listing
November 2018
13 Reads

Hydroalcoholic extract of Cuscuta epithymum enhances pentobarbital-induced sleep: possible involvement of GABAergic system.

Curr Drug Discov Technol 2018 Nov 4. Epub 2018 Nov 4.

Pharmacological Research Center of Medicinal Plants, Mashhad University of Medical Sciences, Mashhad. Iran.

Background: Insomnia is the most common sleep disorder. The present study was undertaken to evaluate the sedative-hypnotic potential of hydroalcoholic extract (HAE) of Cuscuta epithymum and its fractions.

Method: HAE and its fractions including: water fraction (WF), ethyl acetate fraction (EAF) and n-hexan fraction (NHF) were i. Read More

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http://www.eurekaselect.com/167001/article
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http://dx.doi.org/10.2174/1570163815666181105091801DOI Listing
November 2018
12 Reads

Herbal Products Regulations in a few countries - A brief Overview.

Curr Drug Discov Technol 2018 Nov 4. Epub 2018 Nov 4.

Department of Pharmacy Management, Manipal College of Pharmaceutical Sciences, MAHE, Manipal, Karnataka. India.

Herbal medicines have been used by mankind from time immemorial. Moreover, many modern medicines are originated from plant sources. In earlier days, patients were dependent on herbs for treatment and well-being. Read More

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http://dx.doi.org/10.2174/1570163815666181105091254DOI Listing
November 2018
12 Reads

In silico analysis and molecular docking studies of novel 4-Amino-3-(isoquinolin-4-yl)-1H-pyrazolo[3,4-d]pyrimidine derivatives as Dual PI3K/mTOR inhibitors.

Curr Drug Discov Technol 2018 Nov 2. Epub 2018 Nov 2.

Department of Pharmacy, Faculty of Pharmacy, Parul institute of pharmacy, Parul University, Vadodara, Gujarat. India.

mTORC1/ PI3K control multiple anabolic pathways, including protein synthesis, ribosome production, lipogenesis, and nucleotide synthesis, all of which are important for cell and tissue growth.Sapanisertib and Dactolisib inhibit PI3K/AKT/mTOR pathway, an important signalling pathway for many cellular functions such as growth control, metabolism and translation initiation.Dactolisib contain quinolin-3-yl-2,3-dihydroimidazo[4,5-c]quinolin scaffold and Sapanisertib contain benzo[d]oxazol-5-yl-1-ethyl-1H-pyrazolo[3,4-d]pyrimidinnucleous. Read More

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http://dx.doi.org/10.2174/1568009618666181102144934DOI Listing
November 2018
14 Reads

Efficacy of a Herbal Formulation Based on Foeniculum Vulgare in Oligo/Amenorrhea: A Randomized Clinical Trial.

Curr Drug Discov Technol 2018 Oct 29. Epub 2018 Oct 29.

Department of Persian Medicine, School of Persian and Complementary Medicine, Mashhad University of Medical Sciences, Mashhad. Iran.

Background: The aim of this study was to evaluate the efficacy of the herbal tea based on Foeniculum vulgare, on inducing regular bleeding in women with oligomenorrhea and secondary amenorrhea(oligo/amenorrhea).

Methods: Forty women aged 18- 40 with oligo/amenorrhea were enrolled in this randomized controlled clinical trial and were allocated to two groups equally. The women in the first group were treated by Fomentex (Foeniculum vulgare / Mentha longifolia / Vitex agnus-castus) herbal tea 11. Read More

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http://dx.doi.org/10.2174/1570163815666181029120512DOI Listing
October 2018
13 Reads

Docking Studies of Curcumin and Analogues with Various Phosphodiesterase 4 Subtypes.

Curr Drug Discov Technol 2018 Oct 16. Epub 2018 Oct 16.

Faculty of Pharmaceutical Sciences, UCSI University, 1 Jalan Menara Gading, Taman Connaught, Cheras, 56000 Kuala Lumpur. Malaysia.

Introduction: The primary aim of this study is to understand the binding of curcumin and its analogues to different PDE4 subtypes and identification of the role of PDE4 subtype inhibition in the anti-inflammatory property of curcumin. Docking analysis has been used to acquire the above mentioned structural information and this has been further used for designing of curcumin derivatives with better anti-inflammatory activity.

Materials And Method: Curcumin and its analogues were subjected to docking using PDE4A, PDE4B, PDE4C and PDE4D as the target. Read More

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http://dx.doi.org/10.2174/1570163815666181017091655DOI Listing
October 2018
11 Reads

A review article about some herbs affecting vitiligo based on Avicenna's Canon.

Curr Drug Discov Technol 2018 Oct 16. Epub 2018 Oct 16.

Health Department, Mashhad University of Medical Sciences, Mashhad. Iran.

Background: Vitiligo is a pigmentary disorder characterizing by white macules due to loss of melanocytes. Vitiligo affects about 1 to 4% of people around the world. The treatment of vitiligo has a high cost and the long process of treatment in spite of no complete remedy. Read More

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http://dx.doi.org/10.2174/1570163815666181017100847DOI Listing
October 2018
6 Reads

Design, synthesis, characterization of novel linomide analogues and their evaluation for anticancer activity.

Curr Drug Discov Technol 2018 Oct 8. Epub 2018 Oct 8.

Department of Pharmaceutical Chemistry, PES's Rajaram and Tarabai Bandekar College of Pharmacy, Farmagudi, Goa 403401. India.

Background: According to WHO, in 2017, about 90.5 million of people suffer from cancer and about 8.8 million deaths occurred due to disease. Read More

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http://www.eurekaselect.com/166047/article
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http://dx.doi.org/10.2174/1570163815666181008151037DOI Listing
October 2018
13 Reads

Aripiprazole: An FDA Approved Bioactive Compound to treat schizophrenia-A Mini Review.

Curr Drug Discov Technol 2018 Oct 8. Epub 2018 Oct 8.

Central Facility of Instrumentation, School of Pharmaceutical Sciences, IFTM University, Moradabad-244001. India.

Objective: Aripiprazole,a synthetic compound, obtained by chemical modification of the structure of quinolinone is considered as an atypical antipsychotic drug. The present review is an attempt to summarize the updated information related to reported chemistry and pharmacology of Aripiprazole.

Development: Aripiprazole, under development by Otsuka Pharmaceutical, was approved by the U. Read More

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http://dx.doi.org/10.2174/1570163815666181008151718DOI Listing
October 2018
10 Reads

Combiphore (Structure and Ligand based Pharmacophore) Approach for Design of GPR40 Modulators in Management of Diabetes.

Curr Drug Discov Technol 2018 Oct 8. Epub 2018 Oct 8.

Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad 382 481, Gujarat. India.

Pharmacophore mapping and molecular docking can be synergistically integrated to improve the drug design and discovery process. A rational strategy, combiphore approach, derived from the combined study of Structure and Ligand based pharmacophore has been described to identify novel GPR40 modulators. DISCOtech module from Discovery studio was used for the generation of the Structure and Ligand based pharmacophore models which gave hydrophobic aromatic, ring aromatic and negative ionizable as essential pharmacophoric features. Read More

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http://www.eurekaselect.com/166059/article
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http://dx.doi.org/10.2174/1570163815666181008165822DOI Listing
October 2018
2 Reads

Natural Starch in Biomedical and Food Industry: Perception and Overview.

Curr Drug Discov Technol 2018 Oct 3. Epub 2018 Oct 3.

Dept. of Pharmacy, Assam down town University, Panikhaiti, Guwahati, Assam - 781026. India.

Utilization of the native starch is increasing globally because of its wide distribution and occurring naturally. Starch is mainly abundant in tubers and food grains. Scientific research on starch is increasing in recent years due to their unique physiochemical and biomedical properties. Read More

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http://dx.doi.org/10.2174/1570163815666181003143732DOI Listing
October 2018
11 Reads

Herbal Drug Use In Sickle Cell Disease Management; Trends And Perspectives In Sub-Saharan Africa.

Curr Drug Discov Technol 2018 Oct 1. Epub 2018 Oct 1.

Department of Chemical Pathology, Faculty of Basic Clinical Sciences, College of Health Sciences, University of Abuja, P.M.B 117 FCT, Abuja. Nigeria.

Introduction Nigeria has the largest burden of Sickle Cell Disease (SCD) with estimated 100,000 new born affected annually. SCD is a hemoglobin (Hb) disorder with the major form resulting from the substitution of a polar glutamate (Glu) by non-polar Valine (Val) in an invariant region, of Hb chain-subunit. Species of Hb found in sickle cell trait are HbA and HbS at a 60:40 proportion, in SCD only HbS, in the HbC disease only HbC, and in the SC disease it's HbS and HbC in a 50:50 equal proportion. Read More

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http://www.eurekaselect.com/165822/article
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http://dx.doi.org/10.2174/1570163815666181002101611DOI Listing
October 2018
8 Reads

Combined Ligand-Based and Structure-Based Virtual Screening Approach for Identification of New Dipeptidyl Peptidase 4 Inhibitors.

Curr Drug Discov Technol 2018 Sep 26. Epub 2018 Sep 26.

Faculty of Pharmacy, Dharmsinh Desai University, Nadiad, Gujarat. India.

Background: Dipeptidyl Peptidase 4 (DPP 4) enzyme cleaves an incretin based glucoregulatory hormone Glucagon Like Peptide -1 from N-terminal where penultimate amino acid is either alanine or proline. Several DPP 4 inhibitors, "gliptins", are approved for management of Type 2 Diabetes or under clinical trial. In present study, combined pharmacophore and docking based virtual screening protocol was used for identification of new hits from the Specs Database, which would inhibit DPP 4. Read More

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http://www.eurekaselect.com/165681/article
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http://dx.doi.org/10.2174/1570163815666180926111558DOI Listing
September 2018
2 Reads

Do we have a satisfactory cell viability assay? Review of the currently commercially-available assays.

Curr Drug Discov Technol 2018 Sep 24. Epub 2018 Sep 24.

VP Translational Medicine, Biomarkers & Diagnostics Celldex Therapeutics 53 Frontage Road, Suite 220 Hampton, NJ 08827-4032. United States.

Cell-based assays are an important part of the drug discovery process and clinical research. One of the main hurdles is to design sufficiently robust assays with adequate signal to noise parameters while maintaining the inherent physiology of the cells and not interfering with the pharmacology of target being investigated. A plethora of assays that assess cell viability (or cell heath in general) are commercially available and can be classified under different categories according to their concepts and principle of reactions. Read More

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http://dx.doi.org/10.2174/1570163815666180925095433DOI Listing
September 2018
2 Reads

Molecular Docking, G-QSAR studies, Synthesis and Anticancer screening of some New 2-Phenazinamines as Bcr-Abl Tyrosine kinase Inhibitors.

Curr Drug Discov Technol 2018 Sep 13. Epub 2018 Sep 13.

Department of Pharmaceutical Chemistry, Government College of Pharmacy, Aurangabad-431 005, Maharastara. India.

The computational studies on 2-phenazinamines with their protein targets have been carried out to design compounds with potential anticancer activity. This strategy of designing compounds possessing selectivity over specific tyrosine kinase has been achieved through G-QSAR and molecular docking studies. The objective of this research has been to design newer 2-phenazinamine derivatives as Bcr-Abl tyrosine kinase inhibitors by G-QSAR, molecular docking studies followed by wet lab studies along with evaluation of their anticancer potential. Read More

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http://dx.doi.org/10.2174/1570163815666180913122542DOI Listing
September 2018
2 Reads

Cancer Cell Metabolism Featuring Nrf2.

Curr Drug Discov Technol 2018 Sep 10. Epub 2018 Sep 10.

Department of Pharmaceutical Sciences, Western University of Health Sciences, Pomona, CA. United States.

Although the major role of Nrf2 has long been established as a transcription factor for providing cellular protection against oxidative stress, multiple pieces of research and reviews now claim exactly the opposite. The dilemma - "to activate or inhibit" the protein requires an immediate answer, which evidently links cellular metabolism to the causes and purpose of cancer. Profusely growing cancerous cells have prolific energy requirements, which can only be fulfilled by modulating cellular metabolism. Read More

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http://dx.doi.org/10.2174/1570163815666180911092443DOI Listing
September 2018
13 Reads

Synthesis, Characterization and Antimicrobial Evaluation of some N-substituted benzimidazole derivatives.

Curr Drug Discov Technol 2018 Aug 31. Epub 2018 Aug 31.

Faculty of Pharmacy, IFTM University, Moradabad - 244102. India.

Background: Due to the appearance of communicable microbial diseases and the toxicity related with presently used several antimicrobials such as β-lactam antibiotics, tetracyclines, quinolones, macrolides, glycopeptides (vancomycin) etc, demand for new antimicrobial agents has become great concern in new technologies to improve efficacy and safety.

Methods: In search of new antimicrobial agents with higher potency, some N-substituted benzimidazole derivatives (4, 5a-5h & 6) were obtained by chloroacetylation of benzimidazole followed by reaction with different amines which were characterized by spectroscopic methods. All the target compounds were evaluated for their antibacterial and antifungal activity against microorganisms using two fold serial dilution method. Read More

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http://dx.doi.org/10.2174/1570163815666180831164149DOI Listing
August 2018
4 Reads

CoMFA, CoMSIA and HQSAR Analysis of 3-aryl-3-ethoxypropanoic acid derivatives as GPR40 modulators.

Curr Drug Discov Technol 2018 Aug 29. Epub 2018 Aug 29.

Department of Pharmaceutical Analysis, RPCP, Changa. India.

Human GPR40 receptor, also known as free fatty-acid receptor 1, is a G-protein-coupled receptor that binds long chain free fatty acids to enhance glucose-dependent insulin secretion. In order to improve the resistance and efficacy, computational tools were utilized. To build the 3D-QSAR models, CoMFA (Comparative Molecular Field Analysis), CoMSIA (Comparative Molecular Similarity Indices Analysis) and HQSAR (Hologram Quantitative Structure Activity Relationship) were performed on series of 3-aryl-3-ethoxypropanoic acid derivatives. Read More

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http://www.eurekaselect.com/164975/article
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http://dx.doi.org/10.2174/1570163815666180829144431DOI Listing
August 2018
12 Reads

Identification of phenolic compounds from nettle as new candidate inhibitors of main enzymes responsible on type-II diabetes.

Curr Drug Discov Technol 2018 08 28. Epub 2018 Aug 28.

Departement of Chemistry, Faculty of Applied Exacts Sciences, University Ahmed Benbella of Oran, Algeria

Background: In medicinal chemistry, the discovery of small organic molecules that can be optimized and lead to a future drug capable of effectively modulating the biological activity of a therapeutic target remains as major challenge. Because of harmful secondary effects of synthesized therapeutic molecules, the development of research has been oriented towards phytomedicines. Phenolic compounds from medicinal plants are constantly explored for new therapeutic use. Read More

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http://dx.doi.org/10.2174/1570163815666180829094831DOI Listing
August 2018
12 Reads

Antibacterial Flavonoids against Oral Bacteria of Enterococcus faecalis ATCC 29212 from Sarang Semut (Myrmecodia pendans) and its Inhibitor Activity against Enzyme MurA.

Curr Drug Discov Technol 2018 08 27. Epub 2018 Aug 27.

Department of Oral Biology, Faculty of Dentistry , Universitas Padjadjaran-Bandung. Indonesia.

The aim of this work is to isolate antibacterial compounds from Sarang Semut (Myrmecodia pendans) and to evaluate their antibacterial activity against pathogenic oral bacteria of Enterococcus faecalis ATCC 29212 and inhibitory activity against MurA enzyme. The antibacterial compounds from Sarang Semut were isolated by a bioactivity-guided separation method with various solvents and combination of column chromatography on normal and reverse phases. The compounds with concentrations of 1000 and 5000 ppm were assessed against E. Read More

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http://dx.doi.org/10.2174/1570163815666180828113920DOI Listing
August 2018
2 Reads

Topological analysis of electron density in large biomolecular systems.

Curr Drug Discov Technol 2018 Aug 21. Epub 2018 Aug 21.

South Ural State University, Laboratory of Computational Modelling of Drugs, Tchaikovsky str. 20-A, Chelyabinsk. Russian Federation.

AlteQ approach was applied to the tolopogical analysis of electron density for "substrate - cytochrome" complexes. The approach is based on the use of Slater's type atomic contributions. Parameters of the atomic contributions were found using high resolution X-ray diffraction data for organic and inorganic molecules. Read More

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http://dx.doi.org/10.2174/1570163815666180821165330DOI Listing
August 2018
9 Reads

Chemistry And Pharmacological Activities Of Biginelli Product- A Brief Overview.

Curr Drug Discov Technol 2018 08 7. Epub 2018 Aug 7.

Department of Pharmaceutical Chemistry and Analysis, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, Kochi- 682041, Kerala. India.

Dihydropyrimidinones are extremely advantageous small sized molecules owning adaptable pharmaceutical properties. With a molecular formula C4H6N2O, they hold a wide range of biological activities. It is a heterocyclic moiety having two N-atoms at positions 1 and 3. Read More

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http://dx.doi.org/10.2174/1570163815666180807141922DOI Listing
August 2018
16 Reads

Identification and Ranking of Clinical Compounds with Activity against Log-phase Growing Uropathogenic Escherichia coli.

Curr Drug Discov Technol 2018 Aug 7. Epub 2018 Aug 7.

Department of Molecular Microbiology and Immunology, Bloomberg School of Public Health, Johns Hopkins University. United States.

Background: Uropathogenic Escherichia coli (UPEC) is a major cause of urinary tract infections (UTIs). Due to increasing antibiotic-resistance among UPEC bacteria, new treatment options for UTIs are urgently needed.

Objective: To identify new agents targeting growing bacteria that may be used for the treatment of antibiotic-resistant UTIs. Read More

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http://dx.doi.org/10.2174/1570163815666180808115501DOI Listing
August 2018
29 Reads

Identification and Characterization of Chemical Compounds that Inhibit Leucyl-tRNA Synthetase from Pseudomonas aeruginosa.

Curr Drug Discov Technol 2018 Aug 7. Epub 2018 Aug 7.

Chemistry Department, The University of Texas-RGV, 1201 W. University Drive, Edinburg, TX. United States.

Background: Pseudomonas aeruginosa is an opportunistic multi-drug resistance pathogen implicated as the causative agent in a high-percentage of nosocomial and community acquired bacterial infections. The gene encoding leucyl-tRNA synthetase (LeuRS) from P. aeruginosa was overexpressed in Escherichia coli and the resulting protein was characterized. Read More

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http://dx.doi.org/10.2174/1570163815666180808095600DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6367055PMC
August 2018
16 Reads

Effect of geographical location and type of extract on Total phenol/flavon contents and antioxidant activity of different fruits extracts of Withania somnifera.

Curr Drug Discov Technol 2018 Aug 6. Epub 2018 Aug 6.

Department of Pharmaceutical Sciences, H.N.B. Garhwal University (A Central University) Srinagar (Garhwal). India.

Withania somnifera (family solanaceae) is a well investigated medicinal plant which is also called as Indian ginseng due to its wide spectrum of medicinal properties. The contents and activity of the plant may vary depending on the habitat and part of the plant and the solvent used for extraction. The present study deals with the comparative chemical analysis and in vitro antioxidant activity of methanolic fruits extracts and its subfractions (in ethyl acetate, butanol and water) of W. Read More

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http://www.eurekaselect.com/164388/article
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http://dx.doi.org/10.2174/1570163815666180807100456DOI Listing
August 2018
19 Reads

Structure based docking studies of GLUT4 towards exploring selected phytochemicals from Solanum xanthocarpum as a therapeutic target for the treatment of cancer

Curr Drug Discov Technol 2018 08 1. Epub 2018 Aug 1.

Department of Biochemistry, Afe Babalola University, PMB 5454, Ado-Ekiti 360001. Nigeria.

In recent years, there has been an exponential increase in the global burden of cancer which has been associated with several factors including environmental influence, aging, diet, infectious agents, hormonal imbalance and chronic inflammation, among others. Cancerous cells utilize more glucose for its proliferation and survival than normal cells. Thus, the regulation of glucose consumption of cancerous cells through the inhibition of glucose transporter-4-protein (GLUT4) encoded by solute carrier family-2-member-4-gene (Slc2a4) by selected phytochemicals from Somalia xanthocarpum may serve as a new therapeutic candidate for the treatment of cancer. Read More

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http://dx.doi.org/10.2174/1570163815666180801152110DOI Listing
August 2018
9 Reads

A Review on Influence of Spray Drying Process Parameters on the Production of Medicinal Plant Powders.

Curr Drug Discov Technol 2018 Aug 1. Epub 2018 Aug 1.

Departamento de Ingenieria Quimica, UNS, San Juan 670, 8000 Bahia Blanca. Argentina.

Medicinal plants are used by the 80% of the world population as primary health care andthe phytomedicine market is growing exponentially. Currently, the production of phytopharmaceuticals with proper efficacy, safety and consistent quality constitute a relevant challenge. The dried dosage forms of medicinal plants are preferred than liquid presentations because their higher stability. Read More

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http://dx.doi.org/10.2174/1570163815666180801152918DOI Listing
August 2018
12 Reads

Investigation on Quantitative Structure-Activity Relationships of 1,3,4 Oxadiazole Derivatives as Potential Telomerase Inhibitors.

Curr Drug Discov Technol 2018 Jul 23. Epub 2018 Jul 23.

Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF) Universita degli Studi di Palermo, via Archirafi 28, 90123-Palermo. Italy.

A series of 1,3,4-oxadiazole derivatives with significant broad-spectrum anticancer activity against different cell lines, and demonstrated telomerase inhibition, was subjected to Quantitative Structure-Activity Relationships (QSAR) analysis. Validated models with high correlation coefficients were developed. The Multiple Linear Regression (MLR) models, by Ordinary Least Squares (OLS), showed good robustness and predictive capability, according to the Multi-Criteria Decision Making (MCDM = 0. Read More

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http://dx.doi.org/10.2174/1570163815666180724113208DOI Listing
July 2018
14 Reads

Current discovery progress of some emerging anti-infective chalcones: Highlights from 2016 to 2017.

Curr Drug Discov Technol 2018 Jul 20. Epub 2018 Jul 20.

Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya (A Central University), Sagar 470003, Madhya Pradesh. India.

The anti-infective potentials of the natural products are very well known for centuries and are a part of traditional healing. The foremost therapeutic classes include flavones, isoflavones, flavonols, flavanones, flavanols, proanthocyanidins, anthocyanidins, chalcones, and aurones. The chalcone or 1,3-diphenyl-2E-propene-1-one represents the class of natural product which comprise of benzylideneacetophenone function; i. Read More

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http://dx.doi.org/10.2174/1570163815666180720170030DOI Listing
July 2018
9 Reads

Anti-Ophidian Properties Of Herbal Medicinal Plants: Could It Be A Remedy For Snake Bite Envenomation?

Curr Drug Discov Technol 2018 Jul 17. Epub 2018 Jul 17.

Department of Pharmaceutical Technology, Jadavpur University, Kolkata-700032. India.

Snake bite envenoming cause high rates of morbidity and mortality and is one of the serious health related concern all over the globe. Around 3200 species of snakes have been discovered till date. Amid these species, about 1300 species of snakes are venomous. Read More

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http://dx.doi.org/10.2174/1570163815666180718095655DOI Listing
July 2018
2 Reads

Therapeutic potential of Citronella Essential Oil: a review.

Curr Drug Discov Technol 2018 Jul 17. Epub 2018 Jul 17.

Vaish Institute of Pharmaceutical Education and Research, Rohtak-124001. India.

Mosquito borne diseases such as malaria, filariasis, chikunguniya, yellow fever, dengue and Japanese encephalitis are the major cause of remarkable morbidity and mortality in livestock and humans worldwide. Since ancient times, aromatic plants are used for their medicinal value. Essential oils derived from these plants may be used as effective alternatives/adjuvents in pharmaceuticals, biomedical, cosmetic, food, veterinary and agriculture applications. Read More

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http://dx.doi.org/10.2174/1570163815666180718095041DOI Listing
July 2018
5 Reads
1 Citation

Lead optimization studies towards finding NS2B/NS3 protease target-specific inhibitors as potential anti-dengue drug-like compounds.

Curr Drug Discov Technol 2018 Jul 9. Epub 2018 Jul 9.

Department of Computer Science and Engineering, Kalasalingam Academy of Research and Education, Anand Nagar, Krishnankoil. India.

Dengue Fever is a major threatening global health issue caused by a mosquito-borne pathogen. Even though some anti-viral drugs are now available to reduce the disease severity. Still, there is a need for better drug compound to combat with dengue fever. Read More

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http://dx.doi.org/10.2174/1570163815666180709155131DOI Listing
July 2018
9 Reads

Editorial: Thiazole Heterocycle: A Privileged Scaffold for Drug Design and Discovery.

Curr Drug Discov Technol 2018 ;15(3):162

Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T. Road, Phagwara (Punjab) 144411, India.

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http://dx.doi.org/10.2174/157016381503180620153423DOI Listing
January 2018
16 Reads

Appetite reducing herbal drugs from the perspective of Avicenna and Aghili in Iranian Traditional Medicine(Persian medicine).

Curr Drug Discov Technol 2018 Jul 3. Epub 2018 Jul 3.

Department of Traditional Medicine, School of Traditional Medicine, Shahid Beheshti University of Medical Sciences, Tehran, 1516745811. Iran.

The increasing prevalence of obesity is one of the problems of today's society. Man needs food to continue living, activities, and even the metabolism of food and appetite plays an important role in receiving foods, Appetite and weight reducing synthetic drugs are recommended for some patients with high prices and significant side effects, and limited effectiveness in the treatment of obesity. Given the epidemic of obesity and the lack of satisfaction with synthetic drugs these days, people are more likely to use herbal medicines. Read More

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http://dx.doi.org/10.2174/1570163815666180704093151DOI Listing
July 2018
9 Reads

OralAcute and Repeated-Doses Toxicity Study of Valepotriates from Valeriana glechomifolia (Meyer) in Mice.

Curr Drug Discov Technol 2018 Jun 29. Epub 2018 Jun 29.

Laboratorio de Analises Clinicas Veterinarias, Faculdade de Veterinaria, UFRGS, Porto Alegre. Brazil.

Species of Valeriana show sedative, hypnotic, anxiolytic, antidepressant and anti-inflammatory properties, which are associated with valepotriates. However, data about toxicity and safety of these compounds are still limited. The aim of this study was to investigate the toxicity of a valepotriate-enriched fraction (VAL) from Valeriana glechomifolia Meyer based on the Organization for Economic Cooperation and Development (OECD) guidelines 423 and 407. Read More

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http://dx.doi.org/10.2174/1570163815666180629164332DOI Listing
June 2018
3 Reads

Potential drug targets in mycobacterial cell wall: Non-lipid perspective.

Curr Drug Discov Technol 2018 Jun 4. Epub 2018 Jun 4.

Amity Institute of Biotechnology, Amity University Haryana, Gurugram (Manesar)-122413. India.

Tuberculosis (TB) caused by Mycobacterium tuberculosis (MTB), still remains a deadly disease worldwide. With prolonged usage of anti-TB drugs, the current therapeutic regimes are becoming ineffective, particularly due to emergence of drug resistance in MTB. Under such compelling circumstances, it is pertinent to look for new drug targets. Read More

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http://dx.doi.org/10.2174/1570163815666180605113609DOI Listing
June 2018
3 Reads

Oligopeptides for Immunotherapy Approaches in Ovarian Cancer Treatment.

Authors:
Darja Kanduc

Curr Drug Discov Technol 2018 May 24. Epub 2018 May 24.

Department of Biosciences, Biotechnologies & Biopharmaceutics, University of Bari. Italy.

Anti-ovarian cancer vaccines based on minimal immune determinants uniquely expressed in ovarian cancer biomarkers and absent in the human proteome appear to promise a high level of sensitivity and specificity for early ovarian cancer immunodiagnostics, immunoprevention, and immunotherapy. In this context, the present study analyses three ovarian cancer biomarkers - namely sperm surface protein Sp17, WAP four-disulfide core domain protein 2, and müllerian-inhibiting substance - and describes a methodology for constructing ovarian cancer biomarker-derived oligopeptide constructs that might be useful for developing new diagnostic and immunotherapeutic approaches. Read More

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http://dx.doi.org/10.2174/1570163815666180525071740DOI Listing
May 2018
2 Reads