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Synthesis and antidiabetic evaluation of benzimidazole‐tethered 1,2,3‐triazoles
Author(s) -
Deswal Laxmi,
Verma Vikas,
Kumar Devinder,
Kaushik Chander P.,
Kumar Ashwani,
Deswal Yogesh,
Punia Suman
Publication year - 2020
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.202000090
Subject(s) - benzimidazole , chemistry , imidazole , click chemistry , docking (animal) , stereochemistry , azide , proton nmr , active site , triazole , combinatorial chemistry , organic chemistry , enzyme , nursing , medicine
Some novel benzimidazole‐tethered 1,2,3‐triazole derivatives ( 4a–r ) were synthesized by a click reaction between 2‐substituted 1‐(prop‐2‐yn‐1‐yl)‐1 H ‐benzo[ d ]imidazole and in situ azide. The structures of the synthesized compounds were confirmed by spectroscopic studies (one‐ and two‐dimensional nuclear magnetic resonance, Fourier transform infrared, and high‐resolution mass spectra). The synthesized compounds were evaluated for their antidiabetic activity. Compounds 4a – r exhibited a good‐to‐moderate α‐amylase and α‐glucosidase inhibitory activity, with IC 50 values ranging from 0.0410 to 0.0916 µmol/ml and 0.0146 to 0.0732 µmol/ml, respectively. Compounds 4e , 4g , and 4n were found to be most active. Furthermore, the binding conformation of the most active compounds was ascertained by docking studies.