Literature DB >> 31699396

Synthesis, in vitro alpha-glucosidase inhibitory potential of benzimidazole bearing bis-Schiff bases and their molecular docking study.

Fazal Rahim1, Khalid Zaman2, Muhammad Taha3, Hayat Ullah2, Mehreen Ghufran4, Abdul Wadood4, Wajid Rehman2, Nizam Uddin5, Syed Adnan Ali Shah6, Muhammad Sajid7, Faisal Nawaz8, Khalid Mohammed Khan9.   

Abstract

Voglibose and acarbose are distinguished α-glucosidase inhibitors used for controlling of diabetes mellitus. Unfortunately, these distinguished and clinically used inhibitors have also numerous side effects. Subsequently, there is still needed to develop safer therapy. Despite of a broad spectrum of biological importance of benzimidazole, it is occasionally evaluated for α-glucosidase activity. Current study deals with the synthesis and biological screening of benzimidazole bearing bis-Schiff bases (1-19) for their α-glucosidase inhibitory activity. All analogues exhibited excellent to good inhibitory potential (IC50 = 2.20 ± 0.1to 88.60 ± 1.70 µM) when compared with standard drug acarbose (IC50 = 38.45 ± 0.80 µM). A structure activity relationship has been established on the basis of electronic effects and position of different substituents present on phenyl ring. In order to rationalize the binding interactions of most active analogues with the active site of α-glucosidase enzyme, molecular docking study was conducted.
Copyright © 2019 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Benzimidazole; Bis-Schiff bases; Molecular docking; SAR; Synthesis; α-Glucosidase

Mesh:

Substances:

Year:  2019        PMID: 31699396     DOI: 10.1016/j.bioorg.2019.103394

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


  5 in total

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Journal:  Pharmaceuticals (Basel)       Date:  2022-05-27

2.  Design and synthesis of phenoxymethybenzoimidazole incorporating different aryl thiazole-triazole acetamide derivatives as α-glycosidase inhibitors.

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

3.  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

4.  Docking study, molecular dynamic, synthesis, anti-α-glucosidase assessment, and ADMET prediction of new benzimidazole-Schiff base derivatives.

Authors:  Homa Azizian; Keyvan Pedrood; Ali Moazzam; Yousef Valizadeh; Kimia Khavaninzadeh; Ali Zamani; Maryam Mohammadi-Khanaposhtani; Somayeh Mojtabavi; Mohammad Ali Faramarzi; Samanesadat Hosseini; Yaghoub Sarrafi; Hossein Adibi; Bagher Larijani; Hossein Rastegar; Mohammad Mahdavi
Journal:  Sci Rep       Date:  2022-09-01       Impact factor: 4.996

5.  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

  5 in total

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