Literature DB >> 27576293

Molecular docking studies and synthesis of novel bisbenzimidazole derivatives as inhibitors of α-glucosidase.

Musa Özil1, Mustafa Emirik2, Ali Beldüz2, Serdar Ülker3.   

Abstract

A series of bisbenzimidazole derivatives starting from o-phenylenediamine and 4-nitro-o-phenylenediamine were prepared with oxalic acid. Most of the reactions were conducted using both the microwave and conventional methods to compare yields and reaction times. The operational simplicity, environmental friendly conditions and high yield in a significantly short reaction time were the major benefits. All substances' inhibitory activities against α-glucosidase were evaluated. The results may suggest a significant role for the nature of bisbenzimidazole compounds in their inhibitory action against α-glucosidase. They showed different range of α-glucosidase inhibitory potential with IC50 value ranging between 0.44±0.04 and 6.69±0.01μM when compared to the standard acarbose (IC50, 13.34±1.26μM). This has described a new class of α-glucosidase inhibitors. Molecular docking studies were done for all compounds to identify important binding modes responsible for inhibition activity of α-glucosidase.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Bisbenzimidazole; Docking; Microwave; α-Glucosidase

Mesh:

Substances:

Year:  2016        PMID: 27576293     DOI: 10.1016/j.bmc.2016.08.024

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  4 in total

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Authors:  Gajendra Gupta; Yan Sun; Abhishek Das; Peter J Stang; Chang Yeon Lee
Journal:  Coord Chem Rev       Date:  2021-11-22       Impact factor: 22.315

Review 2.  Recent Applications of the Multicomponent Synthesis for Bioactive Pyrazole Derivatives.

Authors:  Diana Becerra; Rodrigo Abonia; Juan-Carlos Castillo
Journal:  Molecules       Date:  2022-07-23       Impact factor: 4.927

3.  Arylsulfonyl histamine derivatives as powerful and selective α-glucosidase inhibitors.

Authors:  M I Osella; M O Salazar; M D Gamarra; D M Moreno; F Lambertucci; D E Frances; R L E Furlan
Journal:  RSC Med Chem       Date:  2020-03-12

4.  Design, synthesis, molecular docking, and in vitro α-glucosidase inhibitory activities of novel 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines against yeast and rat α-glucosidase.

Authors:  Fariba Peytam; Ghazaleh Takalloobanafshi; Toktam Saadattalab; Maryam Norouzbahari; Zahra Emamgholipour; Setareh Moghimi; Loghman Firoozpour; Hamid Reza Bijanzadeh; Mohammad Ali Faramarzi; Somayeh Mojtabavi; Parviz Rashidi-Ranjbar; Saeed Karima; Roya Pakraad; Alireza Foroumadi
Journal:  Sci Rep       Date:  2021-06-07       Impact factor: 4.379

  4 in total

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