Literature DB >> 31838286

Synthesis and biological evaluation of new benzimidazole-1,2,3-triazole hybrids as potential α-glucosidase inhibitors.

Nafise Asemanipoor1, Maryam Mohammadi-Khanaposhtani2, Shahram Moradi1, Mahbobeh Vahidi3, Mehdi Asadi4, Mohammad Ali Faramarzi3, Mohammad Mahdavi5, Mahmood Biglar6, Bagher Larijani6, Haleh Hamedifar7, Mir Hamed Hajimiri8.   

Abstract

In this study, a series of benzimidazole-1,2,3-triazole hybrids 8a-n as new α-glucosidase inhibitors were designed and synthesized. In vitro α-glucosidase inhibition activity results indicated that all the synthesized compounds (IC50 values ranging from 25.2 ± 0.9 to 176.5 ± 6.7 μM) exhibited more inhibitory activity in comparison to standard drug acarbose (IC50 = 750.0 ± 12.5 μM). Enzyme kinetic study on the most potent compound 8c revealed that this compound was a competitive inhibitor into α-glucosidase. Moreover, the docking study was performed in order to evaluation of interaction modes of the synthesized compounds in the active site of α-glucosidase and to explain structure-activity relationships of the most potent compounds and their corresponding analogs.
Copyright © 2019 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  1,2,3-Triazole; Benzimidazole; Molecular docking; α-Glucosidase inhibitor

Mesh：

Substances：

Year:  2019        PMID： 31838286     DOI： 10.1016/j.bioorg.2019.103482

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


  6 in total

1.  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

2.  Cyanoacetohydrazide linked to 1,2,3-triazole derivatives: a new class of α-glucosidase inhibitors.

Authors:  Aida Iraji; Diba Shareghi-Brojeni; Somayeh Mojtabavi; Mohammad Ali Faramarzi; Tahmineh Akbarzadeh; Mina Saeedi
Journal:  Sci Rep       Date:  2022-05-23       Impact factor: 4.996

3.  Design, synthesis, biological evaluation, and molecular modeling studies of pyrazole-benzofuran hybrids as new α-glucosidase inhibitor.

Authors:  Fateme Azimi; Homa Azizian; Mohammad Najafi; Ghadamali Khodarahmi; Lotfollah Saghaei; Motahareh Hassanzadeh; Jahan B Ghasemi; Mohammad Ali Faramarzi; Bagher Larijani; Farshid Hassanzadeh; Mohammad Mahdavi
Journal:  Sci Rep       Date:  2021-10-21       Impact factor: 4.379

4.  α-Glucosidase and α-Amylase Inhibitory Potentials of Quinoline-1,3,4-oxadiazole Conjugates Bearing 1,2,3-Triazole with Antioxidant Activity, Kinetic Studies, and Computational Validation.

Authors:  Nosipho Cele; Paul Awolade; Pule Seboletswe; Kolawole Olofinsan; Md Shahidul Islam; Parvesh Singh
Journal:  Pharmaceuticals (Basel)       Date:  2022-08-22

5.  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

6.  Inhibitory Effect of Fisetin on α-Glucosidase Activity: Kinetic and Molecular Docking Studies.

Authors:  Beiyun Shen; Xinchen Shangguan; Zhongping Yin; Shaofu Wu; Qingfeng Zhang; Wenwen Peng; Jingen Li; Lu Zhang; Jiguang Chen
Journal:  Molecules       Date:  2021-08-31       Impact factor: 4.411
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.