Literature DB >> 31911306

Synthesis, α-glycosidase inhibitory potential and molecular docking study of benzimidazole derivatives.

Muhammad Taha1, Fazal Rahim2, Khalid Zaman2, Manikandan Selvaraj3, Nizam Uddin4, Rai Khalid Farooq5, Muhammad Nawaz6, Muhammad Sajid7, Faisal Nawaz8, Mohamad Ibrahim9, Khalid Mohammed Khan10.   

Abstract

A series of twenty-six analogs of benzimidazole based oxadiazole have been synthesized and evaluated against alpha-glycosidase enzyme. Most the analogs showed excellent to good inhibitory potential. Among the screened analogs, analog 1, 2, 3 and 14 with IC50 values 4.6 ± 0.1, 9.50 ± 0.3, 2.6 ± 0.1 and 9.30 ± 0.4 µM respectively showedexcellent inhibitory potential than reference drug acarbose (IC50 = 38.45 ± 0.80 µM). Some of the analogs like 19, 21, 22 and 23 with methyl and methoxy substituent on phenyl ring show hydrophobic interaction and were found with no inhibitory potential. The binding interactions between synthesized analogs and ligands protein were confirmed through molecular docking study. Various spectroscopic techniques like 1H NMR, 13C NMR, and EI-MS were used for characterization of all synthesized analogs. These derivatives were synthesized by simple mode of synthesis like heterocyclic ring formation.
Copyright © 2019 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Benzimidazole; Molecular docking; Oxadiazole; Synthesis; α-glycosidase inhibition

Mesh:

Substances:

Year:  2019        PMID: 31911306     DOI: 10.1016/j.bioorg.2019.103555

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


  6 in total

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Authors:  Anita Nasli Esfahani; Aida Iraji; Amir Alamir; Shahram Moradi; Mohammad Sadegh Asgari; Samanesadat Hosseini; Somayeh Mojtabavi; Ensieh Nasli-Esfahani; Mohammad Ali Faramarzi; Fatemeh Bandarian; Bagher Larijani; Haleh Hamedifar; Mir Hamed Hajimiri; Mohammad Mahdavi
Journal:  Mol Divers       Date:  2021-09-13       Impact factor: 3.364

2.  Bioactivity-guided separation of potential α-glycosidase inhibitor from clerodendranthus spicatus based on HSCCC coupled with molecular docking.

Authors:  Chunsheng Zhu; Hongjuan Niu; Anzheng Nie; Meng Bian
Journal:  Sci Rep       Date:  2021-03-25       Impact factor: 4.379

Review 3.  Heterocyclic compounds as a magic bullet for diabetes mellitus: a review.

Authors:  Umme Farwa; Muhammad Asam Raza
Journal:  RSC Adv       Date:  2022-08-16       Impact factor: 4.036

Review 4.  Research progress on the synthesis and pharmacology of 1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives: a mini review.

Authors:  Jing-Jing Wang; Wen Sun; Wei-Dong Jia; Ming Bian; Li-Jun Yu
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

5.  Synthesis of Novel Benzimidazole-Based Thiazole Derivatives as Multipotent Inhibitors of α-Amylase and α-Glucosidase: In Vitro Evaluation along with Molecular Docking Study.

Authors:  Rafaqat Hussain; Shahid Iqbal; Mazloom Shah; Wajid Rehman; Shoaib Khan; Liaqat Rasheed; Fazal Rahim; Ayed A Dera; Sana Kehili; Eslam B Elkaeed; Nasser S Awwad; Majed A Bajaber; Mohammed Issa Alahmdi; Hamad Alrbyawi; Hashem O Alsaab
Journal:  Molecules       Date:  2022-09-30       Impact factor: 4.927

6.  Synthesis of Benzimidazole-Based Analogs as Anti Alzheimer's Disease Compounds and Their Molecular Docking Studies.

Authors:  Bushra Adalat; Fazal Rahim; Muhammad Taha; Foziah J Alshamrani; El Hassane Anouar; Nizam Uddin; Syed Adnan Ali Shah; Zarshad Ali; Zainul Amiruddin Zakaria
Journal:  Molecules       Date:  2020-10-20       Impact factor: 4.411

  6 in total

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