Journal ArticleDOI
Synthesis, α-glucosidase inhibitory activity and in silico study of tris-indole hybrid scaffold with oxadiazole ring: As potential leads for the management of type-II diabetes mellitus.
Muhammad Taha,Fazal Rahim,Syahrul Imran,Nor Hadiani Ismail,Hayat Ullah,Manikandan Selvaraj,Muhammad Javid,Uzma Salar,Muhammad Ali,Khalid Mohammed Khan +9 more
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TLDR
Novel tris-indole-oxadiazole hybrid analogs (1-21), structurally characterized by various spectroscopic techniques such as 1H NMR, EI-MS, and 13C NMR are synthesized, showing that almost all compounds in this series indicate the drug aptness.About:
This article is published in Bioorganic Chemistry.The article was published on 2017-10-01. It has received 68 citations till now. The article focuses on the topics: Docking (molecular) & Acarbose.read more
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Medicinal chemistry of indole derivatives: Current to future therapeutic prospectives.
Archana Kumari,Rajesh K. Singh +1 more
TL;DR: This review summarizes some of the recent effective chemical synthesis (2014-2018) for indole ring and emphasized on the structure-activity relationship (SAR) to reveal the active pharmacophores of various indole analogues accountable for anticancer, anticonvulsant, antimicrobial, antitubercular, antimalarial, antiviral, antidiabetic and other miscellaneous activities which have been investigated in the last five years.
Journal ArticleDOI
Recent advance in oxazole-based medicinal chemistry.
TL;DR: This work systematically reviewed the recent researches and developments of the whole range of oxazole compounds as medicinal drugs, including antibacterial, antifungal, antiviral, antitubercular, anticancer, anti-inflammatory and analgesic, antidiabetic, antiparasitic, anti -obesitic,Anti-neuropathic, antioxidative as well as other biological activities.
Journal ArticleDOI
Synthetic heterocyclic candidates as promising α-glucosidase inhibitors: An overview.
Manoj Dhameja,Preeti Gupta +1 more
TL;DR: This review deals with recently discovered heterocyclic molecules that have been evaluated to exhibit inhibition of α-glucosidase enzyme in the treatment of type 2 diabetes mellitus.
Journal ArticleDOI
Anti-diabetic drugs recent approaches and advancements
TL;DR: This review summarises recent approaches and advancement in anti-diabetes treatment concerning characteristics, structure-activity relationships, functional mechanisms, expression regulation, and applications in medicine.
Journal ArticleDOI
Bisindolylmethane thiosemicarbazides as potential inhibitors of urease: Synthesis and molecular modeling studies.
Muhammad Taha,Hayat Ullah,Laode Muhammad Ramadhan Al Muqarrabun,Muhammad Naseem Khan,Fazal Rahim,Norizan Ahmat,Muhammad Javid,Muhammad Ali,Khalid Mohammed Khan +8 more
TL;DR: Bisindolylmethane thiosemicarbazides 1-18 were synthesized, characterized by 1H NMR and ESI MS and evaluated for urease inhibitory potential and analog 9 with di-chloro substitution on phenyl ring was identified as the most potent inhibitor of Urease.
References
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Journal ArticleDOI
Improved protein-ligand docking using GOLD.
Marcel L. Verdonk,Jason C. Cole,Michael J. Hartshorn,Christopher W. Murray,Richard D. Taylor +4 more
TL;DR: In terms of producing binding energy estimates, the Goldscore function appears to perform better than the Chemscore function and the two consensus protocols, particularly for faster search settings.
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Global Estimates for Prevalence of Diabetes Mellitus and Impaired Glucose Tolerance in Adults
Hilary King,Marian Rewers +1 more
TL;DR: Diabetes in adults is now a global health problem, and populations of developing countries, minority groups, and disadvantaged communities in industrialized countries now face the greatest risk.
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Prediction of Properties from Simulations: Free Energies of Solvation in Hexadecane, Octanol, and Water
TL;DR: In this article, Monte Carlo statistical mechanics simulations have been carried out for more than 200 organic solutes, including 125 drugs and related heterocycles, in aqueous solution, using the OPLS-AA force field augmented with CM1P partial charges.
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Miglitol: a review of its therapeutic potential in type 2 diabetes mellitus.
TL;DR: In long term, well designed trials miglitol reduces fasting and postprandial plasma glucose levels, thus improving glycaemic control, which is reflected in a reduced HbA1c level in patients with type 2 diabetes mellitus.
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Effect of two α-glucosidase inhibitors, voglibose and acarbose, on postprandial hyperglycemia correlates with subjective abdominal symptoms
TL;DR: The results demonstrated that 50 mg acarbose and 0.3 mg voglibose had similar overall effects on postprandial hyperglycemia as well as subjective symptoms, but marked interindividual variation existed.