Literature DB >> 28189421

Synthesis, molecular docking and α-glucosidase inhibition of 2-((5,6-diphenyl-1,2,4-triazin-3-yl)thio)-N-arylacetamides.

Guangcheng Wang1, Xin Li2, Jing Wang2, Zhenzhen Xie2, Luyao Li2, Ming Chen2, Shan Chen2, Yaping Peng2.   

Abstract

A novel series of 2-((5,6-diphenyl-1,2,4-triazin-3-yl)thio)-N-arylacetamides 5a-5q have been synthesized and evaluated for their α-glucosidase inhibitory activity. All newly synthesized compounds exhibited potent α-glucosidase inhibitory activity in the range of IC50=12.46±0.13-72.68±0.20μM, when compared to the standard drug acarbose (IC50=817.38±6.27μM). Among the series, compound 5j (12.46±0.13μM) with strong electron-withdrawing nitro group on the arylacetamide moiety was identified as the most potent inhibitor of α-glucosidase. Molecular docking study was carried out to explore the binding interactions of these compounds with α-glucosidase. Our study identifies a novel series of potent α-glucosidase inhibitors for further investigation.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  1,2,4-Triazine; Molecular docking; α-Glucosidase inhibitor

Mesh:

Substances:

Year:  2017        PMID: 28189421     DOI: 10.1016/j.bmcl.2017.01.094

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Synthesis, characterization, antibacterial evaluation, 2D-QSAR modeling and molecular docking studies for benzocaine derivatives.

Authors:  Israa Taha; Eman M Keshk; Abdel-Galil M Khalil; Ahmed Fekri
Journal:  Mol Divers       Date:  2020-09-25       Impact factor: 2.943

2.  Discovery of 5,6-diaryl-1,2,4-triazines hybrids as potential apoptosis inducers.

Authors:  Dong-Jun Fu; Jian Song; Yu-Hui Hou; Ruo-Han Zhao; Jia-Huan Li; Ruo-Wang Mao; Jia-Jia Yang; Ping Li; Xiao-Lin Zi; Zhong-Hua Li; Qing-Qing Zhang; Fei-Yan Wang; Sai-Yang Zhang; Yan-Bing Zhang; Hong-Min Liu
Journal:  Eur J Med Chem       Date:  2017-07-08       Impact factor: 6.514

3.  Study on the interaction of triaryl-dihydro-1,2,4-oxadiazoles with α-glucosidase.

Authors:  Arefeh Khosravi; Gholamhassan Vaezi; Vida Hojati; Khosrou Abdi
Journal:  Daru       Date:  2020-01-06       Impact factor: 3.117

4.  Two New Compounds Containing Pyridinone or Triazine Heterocycles Have Antifungal Properties against Candida albicans.

Authors:  Laura Mena; Muriel Billamboz; Rogatien Charlet; Bérangère Desprès; Boualem Sendid; Alina Ghinet; Samir Jawhara
Journal:  Antibiotics (Basel)       Date:  2022-01-08
  4 in total

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