Literature DB >> 34481854

Synthesis of indole derivatives as diabetics II inhibitors and enzymatic kinetics study of α-glucosidase and α-amylase along with their in-silico study.

Muhammad Taha1, Ahlam Sayer Alrashedy2, Noor Barak Almandil3, Naveed Iqbal4, El Hassane Anouar5, Muhammad Nawaz6, Nizam Uddin7, Sridevi Chigurupati8, Abdul Wadood9, Fazal Rahim10, Suprava Das11, Vijayan Venugopal12, Faisal Nawaz13, Khalid Mohammed Khan14.   

Abstract

In this study, we have investigated a series of indole-based compounds for their inhibitory study against pancreatic α-amylase and intestinal α-glucosidase activity. Inhibitors of carbohydrate degrading enzymes appear to have an essential role as antidiabetic drugs. All analogous exhibited good to moderate α-amylase (IC50 = 3.80 to 47.50 μM), and α-glucosidase inhibitory interactions (IC50 = 3.10-52.20 μM) in comparison with standard acarbose (IC50 = 12.28 μM and 11.29 μM). The analogues 4, 11, 12, 15, 14 and 17 had good activity potential both for enzymes inhibitory interactions. Structure activity relationships were deliberated to propose the influence of substituents on the inhibitory potential of analogues. Docking studies revealed the interaction of more potential analogues and enzyme active site. Further, we studied their kinetic study of most active compounds showed that compounds 15, 14, 12, 17 and 11 are competitive for α-amylase and non- competitive for α-glucosidase.
Copyright © 2021 Elsevier B.V. All rights reserved.

Entities:  

Keywords:  Indole analogues; Intestinal α-glucosidase enzymes interactions; Kinetic study; Pancreatic α-amylase

Mesh:

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Year:  2021        PMID: 34481854     DOI: 10.1016/j.ijbiomac.2021.08.207

Source DB:  PubMed          Journal:  Int J Biol Macromol        ISSN: 0141-8130            Impact factor:   6.953


  2 in total

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Authors:  Kirana P Mugaranja; Ananda Kulal
Journal:  Heliyon       Date:  2022-05-02

2.  Synthesis and Evaluation of 1,3,5-Triaryl-2-Pyrazoline Derivatives as Potent Dual Inhibitors of Urease and α-Glucosidase Together with Their Cytotoxic, Molecular Modeling and Drug-Likeness Studies.

Authors:  Rabia Mehmood; Amina Sadiq; Reem I Alsantali; Ehsan Ullah Mughal; Meshari A Alsharif; Nafeesa Naeem; Asif Javid; Munirah M Al-Rooqi; Gul-E-Saba Chaudhry; Saleh A Ahmed
Journal:  ACS Omega       Date:  2022-01-20
  2 in total

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