Design and Synthesis of Phenoxymethybenzoimidazole Incorporating Different Aryl Thiazole-triazole Acetamide Derivatives As α-glycosidase Inhibitors

Overview

Journal Mol Divers

Date 2021 Sep 13

PMID 34515954

Citations 12

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

Affiliations

Soon will be listed here.

Abstract

A novel series of phenoxymethybenzoimidazole derivatives (9a-n) were rationally designed, synthesized, and evaluated for their α-glycosidase inhibitory activity. All tested compounds displayed promising α-glycosidase inhibitory potential with IC values in the range of 6.31 to 49.89 μM compared to standard drug acarbose (IC = 750.0 ± 10.0 μM). Enzyme kinetic studies on 9c, 9g, and 9m as the most potent compounds revealed that these compounds were uncompetitive inhibitors into α-glycosidase. Docking studies confirmed the important role of benzoimidazole and triazole rings of the synthesized compounds to fit properly into the α-glycosidase active site. This study showed that this scaffold can be considered as a highly potent α-glycosidase inhibitor.

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