Design, synthesis, in vitro, and in silico studies of novel diarylimidazole-1,2,3-triazole hybrids as potent α-glucosidase inhibitors

Blanca Corona

doi:10.1016/j.bmc.2019.115148

Design, synthesis, in vitro, and in silico studies of novel diarylimidazole-1,2,3-triazole hybrids as potent α-glucosidase inhibitors

2019-12-01

41

PRE

AI

M

Maryam Mohammadi‐Khanaposhtani

M

Mohammad Asgari

N

Nafiseh Eghbalnejad

M

Mohammad Ali Faramarzi

B

Bagher Larijani

M

Mohammad Mahdavi

T

Tahmineh Akbarzadeh *

DOI：10.1016/j.bmc.2019.115148

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Abstract

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In this work, new derivatives of diarylimidazole-1,2,3-triazole 7a-p were designed, synthesized, and evaluated for their in vitro alpha-glucosidase inhibitory activity. All compounds showed potent inhibitory activity in the range of IC50 = 90.4-246.7 mu M comparing with acarbose as the standard drug (IC50 = 750.0 mu M). Among the synthesized compounds, compounds 7b, 7c, and 7e were approximately 8 times more potent than acarbose. The kinetic study of those compounds indicated that they acted as the competitive inhibitors of alpha-glucosidase. Molecular docking studies were also carried out for compounds 7b, 7c, and 7e using modeled alpha-glucosidase to find the interaction modes responsible for the desired inhibitory activity.

Keywords:

Diarylimidazole

Docking study

alpha-Glucosidase inhibitors

Kinetic study

1,2,3-triazole

Design, synthesis, in vitro, and in silico studies of novel diarylimidazole-1,2,3-triazole hybrids as potent α-glucosidase inhibitors

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