Literature DB >> 25528720

Triazinoindole analogs as potent inhibitors of α-glucosidase: synthesis, biological evaluation and molecular docking studies.

Fazal Rahim1, Khadim Ullah2, Hayat Ullah2, Abdul Wadood3, Muhammad Taha4, Ashfaq Ur Rehman3, Imad uddin2, Muhammad Ashraf5, Ayesha Shaukat5, Wajid Rehman2, Shafqat Hussain6, Khalid Mohammed Khan6.   

Abstract

A new series of triazinoindole analogs 1-11 were synthesized, characterized by EI-MS and (1)H NMR, evaluated for α-glucosidase inhibitory potential. All eleven (11) analogs showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 2.46±0.008 and 312.79±0.06 μM when compared with the standard acarbose (IC50, 38.25±0.12 μM). Among the series, compounds 1, 3, 4, 5, 7, 8, and 11 showed excellent inhibitory potential with IC50 values 2.46±0.008, 37.78±0.05, 28.91±0.0, 38.12±0.04, 37.43±0.03, 36.89±0.06 and 37.11±0.05 μM respectively. All other compounds also showed good enzyme inhibition. The binding modes of these analogs were confirmed through molecular docking.
Copyright © 2014 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Molecular docking; Synthesis; Triazinoindole; α-Glucosidase inhibition

Mesh:

Substances:

Year:  2014        PMID: 25528720     DOI: 10.1016/j.bioorg.2014.12.001

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  6 in total

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5.  Synthesis of Novel Triazinoindole-Based Thiourea Hybrid: A Study on α-Glucosidase Inhibitors and Their Molecular Docking.

Authors:  Muhammad Taha; Foziah J Alshamrani; Fazal Rahim; Shawkat Hayat; Hayat Ullah; Khalid Zaman; Syahrul Imran; Khalid Mohammed Khan; Farzana Naz
Journal:  Molecules       Date:  2019-10-23       Impact factor: 4.411

6.  Inhibitory Effect of Fisetin on α-Glucosidase Activity: Kinetic and Molecular Docking Studies.

Authors:  Beiyun Shen; Xinchen Shangguan; Zhongping Yin; Shaofu Wu; Qingfeng Zhang; Wenwen Peng; Jingen Li; Lu Zhang; Jiguang Chen
Journal:  Molecules       Date:  2021-08-31       Impact factor: 4.411

  6 in total

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