Literature DB >> 26162519

Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase.

Fazal Rahim1, Hayat Ullah2, Muhammad Tariq Javid2, Abdul Wadood3, Muhammad Taha4, Muhammad Ashraf5, Ayesha Shaukat5, Muhammad Junaid3, Shafqat Hussain6, Wajid Rehman2, Rashad Mehmood7, Muhammad Sajid8, Muhammad Naseem Khan2, Khalid Mohammed Khan6.   

Abstract

A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and (1)H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23±0.03 and 424.41±0.94μM when compared with the standard acarbose (IC50, 38.25±0.12μM). Compound (8) (IC50, 18.23±0.03μM) and compound (7) (IC50=36.75±0.05μM) exhibited outstanding inhibitory potential much better than the standard acarbose (IC50, 38.25±0.12μM). All other analogs also showed good to moderate enzyme inhibition. Molecular docking studies were carried out in order to find the binding affinity of thiazole derivatives with enzyme. Studies showed these thiazole analogs as a new class of α-glucosidase inhibitors.
Copyright © 2015 Elsevier Inc. All rights reserved.

Entities:  

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

Mesh:

Substances:

Year:  2015        PMID: 26162519     DOI: 10.1016/j.bioorg.2015.06.006

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


  6 in total

1.  Synthesis, in vitro [Formula: see text]-glucosidase inhibitory activity, and in silico study of (E)-thiosemicarbazones and (E)-2-(2-(arylmethylene)hydrazinyl)-4-arylthiazole derivatives.

Authors:  Muhammad Ali; Khalid Mohammed Khan; Uzma Salar; Mohammed Ashraf; Muhammad Taha; Abdul Wadood; Sujhla Hamid; Muhammad Riaz; Basharat Ali; Shahbaz Shamim; Farman Ali; Shahnaz Perveen
Journal:  Mol Divers       Date:  2018-05-29       Impact factor: 2.943

2.  Bio-Oriented Synthesis of Novel (S)-Flurbiprofen Clubbed Hydrazone Schiff's Bases for Diabetic Management: In Vitro and In Silico Studies.

Authors:  Aftab Alam; Mumtaz Ali; Najeeb Ur Rehman; Saeed Ullah; Sobia Ahsan Halim; Abdul Latif; Ajmal Khan; Obaid Ullah; Shujaat Ahmad; Ahmed Al-Harrasi; Manzoor Ahmad
Journal:  Pharmaceuticals (Basel)       Date:  2022-05-27

3.  Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase Inhibitors.

Authors:  Zhenzhen Xie; Guangcheng Wang; Jing Wang; Ming Chen; Yaping Peng; Luyao Li; Bing Deng; Shan Chen; Wenbiao Li
Journal:  Molecules       Date:  2017-04-20       Impact factor: 4.411

4.  Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor.

Authors:  Muhammad Taha; Fazal Rahim; Aftab Ahmad Khan; El Hassane Anouar; Naveed Ahmed; Syed Adnan Ali Shah; Mohamed Ibrahim; Zainul Amiruddin Zakari
Journal:  Sci Rep       Date:  2020-05-14       Impact factor: 4.379

5.  Structure and inhibition of Cryptococcus neoformans sterylglucosidase to develop antifungal agents.

Authors:  Nivea Pereira de Sa; Adam Taouil; Jinwoo Kim; Timothy Clement; Reece M Hoffmann; John E Burke; Robert C Rizzo; Iwao Ojima; Maurizio Del Poeta; Michael V Airola
Journal:  Nat Commun       Date:  2021-10-07       Impact factor: 17.694

6.  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 in total

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