Literature DB >> 33756236

Evaluation and docking of indole sulfonamide as a potent inhibitor of α-glucosidase enzyme in streptozotocin -induced diabetic albino wistar rats.

Muhammad Taha1, Syahrul Imran2, Mohammed Salahuddin3, Naveed Iqbal4, Fazal Rahim5, Nizam Uddin6, Adeeb Shehzad3, Rai Khalid Farooq7, Munther Alomari8, Khalid Mohammed Khan9.   

Abstract

We have synthesized new hybrid class of indole bearing sulfonamide scaffolds (1-17) as α-glucosidase inhibitors. All scaffolds were found to be active except scaffold 17 and exhibited IC50 values ranging from 1.60 to 51.20 µM in comparison with standard acarbose (IC50 = 42.45 µM). Among the synthesized hybrid class scaffolds 16 was the most potent analogue with IC50 value 1.60 μM, showing many folds better potency as compared to standard acarbose. Whereas, synthesized scaffolds 1-15 showed good α-glucosidase inhibitory potential. Based on α-glucosidase inhibitory effect, Scaffold 16 was chosen due to highest activity in vitro for further evaluation of antidiabetic activity in Streptozotocin induced diabetic rats. The Scaffold 16 exhibited significant antidiabetic activity. All analogues were characterized through 1H, 13CNMR and HR MS. Structure-activity relationship of synthesized analogues was established and confirmed through molecular docking study.
Copyright © 2021 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  In vivo; Indole analogs; Molecular docking; SAR; α-Glucosidase inhibitors

Year:  2021        PMID: 33756236     DOI: 10.1016/j.bioorg.2021.104808

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


  2 in total

1.  Antidiabetic, antioxidant, and anti-obesity effects of phenylthio-ethyl benzoate derivatives, and molecular docking study regarding α-amylase enzyme.

Authors:  Nidal Jaradat; Ahmad Khasati; Maram Hawi; Mohammed Hawash; Suhaib Shekfeh; Mohammad Qneibi; Ahmad M Eid; Mohammad Arar; Mohammed T Qaoud
Journal:  Sci Rep       Date:  2022-02-24       Impact factor: 4.379

2.  Synthesis of Novel 2,3-Dihydro-1,5-Benzothiazepines as α-Glucosidase Inhibitors: In Vitro, In Vivo, Kinetic, SAR, Molecular Docking, and QSAR Studies.

Authors:  Rabia Mehmood; Ehsan Ullah Mughal; Eslam B Elkaeed; Rami J Obaid; Yasir Nazir; Hanan A Al-Ghulikah; Nafeesa Naeem; Munirah M Al-Rooqi; Saleh A Ahmed; Syed Wadood Ali Shah; Amina Sadiq
Journal:  ACS Omega       Date:  2022-08-17
  2 in total

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