Literature DB >> 25955493

Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies.

Fazal Rahim1, Fazal Malik2, Hayat Ullah2, Abdul Wadood3, Fahad Khan2, Muhammad Tariq Javid2, Muhammad Taha4, Wajid Rehman2, Ashfaq Ur Rehman3, Khalid Mohammed Khan5.   

Abstract

Isatin base Schiff bases (1-20) were synthesized, characterized by (1)H NMR and EI/MS and evaluated for α-glucosidase inhibitory potential. Out of these twenty (20) compounds only six analogs showed potent α-glucosidase inhibitory potential with IC50 value ranging in between 2.2±0.25 and 83.5±1.0μM when compared with the standard acarbose (IC50=840±1.73μM). Among the series compound 2 having IC50 value (18.3±0.56μM), 9 (83.5±1.0μM), 11 (3.3±0.25μM), 12 (2.2±0.25μM), 14 (11.8±0.15μM), and 20 (3.0±0.15μM) showed excellent inhibitory potential many fold better than the standard acarbose. The binding interactions of these active analogs were confirmed through molecular docking.
Copyright © 2015 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Isatin; Molecular docking; Schiff bases; Synthesis; α-Glucosidase inhibition

Mesh：

Substances：

Year:  2015        PMID： 25955493     DOI： 10.1016/j.bioorg.2015.03.005

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


  9 in total

1.  Intramolecular versus intermolecular hydrogen bonds in a novel conjugated dimethylamino-benzylidene-amino-2-naphthoic acid Schiff base.

Authors:  Ibrahim Ahmed Z Al-Ansari
Journal:  J Mol Model       Date:  2017-06-30       Impact factor: 1.810

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

Review 3.  Exploration of the Detailed Structure-Activity Relationships of Isatin and Their Isomers As Monoamine Oxidase Inhibitors.

Authors:  Sunil Kumar; Aathira Sujathan Nair; Mohamed A Abdelgawad; Bijo Mathew
Journal:  ACS Omega       Date:  2022-05-05

Review 4.  Isatin and its derivatives: a survey of recent syntheses, reactions, and applications.

Authors:  Rita Kakkar
Journal:  Medchemcomm       Date:  2019-01-15       Impact factor: 3.597

5.  Synthesis, α-glucosidase inhibition and molecular docking studies of novel thiazolidine-2,4-dione or rhodanine derivatives.

Authors:  Guang-Cheng Wang; Ya-Ping Peng; Zhen-Zhen Xie; Jing Wang; Ming Chen
Journal:  Medchemcomm       Date:  2017-05-31       Impact factor: 3.597

6.  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

7.  Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors.

Authors:  Zipeng Gong; Zhenzhen Xie; Jie Qiu; Guangcheng Wang
Journal:  Molecules       Date:  2017-10-30       Impact factor: 4.411

8.  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

9.  Induction of anxiolytic, antidepressant and analgesic effects by Shiff base of (E)-3-(1H-imidazol-4-yl)-2-((2-oxoindolin-3-ylidene)amino)propanoic acid derivatives in diabetic rats.

Authors:  Mohaddese Goleij; Leila Youseftabar-Miri; Maryam Montazeri; Fatemeh Khakpai
Journal:  J Diabetes Metab Disord       Date:  2021-01-03
  9 in total

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