Synthesis and molecular docking study of some 5,6-dichloro-2-cyclopropyl-1H-benzimidazole derivatives bearing triazole, oxadiazole, and imine functionalities as potent inhibitors of urease

Bioorganic & Medicinal Chemistry Letters
Emre MenteşeBahittin Kahveci

Abstract

A new series of benzimidazole compounds including hydrazinecarbothioamide, 1,2,4-triazole, 1,3,4-oxadiazole and imine function were synthesized starting from 5,6-dichloro-2-cyclopropyl-1H-benzimidazole. All of the benzimidazole derivatives exhibited good urease inhibitor activity. Compound 6a proved to be the most potent showing an enzyme inhibitory activity with an IC50=0.06µM. Molecular docking studies were also conducted on enzyme extracted from Jack bean urease to identify the binding mode of the newly synthesized compounds.

Citations

Oct 31, 2018·Archiv der Pharmazie·Emre MenteşeMustafa Emirik
Mar 22, 2019·Current Protein & Peptide Science·Ritu Kataria, Anurag Khatkar
May 16, 2020·Scientific Reports·Muhammad TahaZainul Amiruddin Zakari
Feb 20, 2019·Expert Opinion on Therapeutic Patents·Abdul HameedKhalid Mohammed Khan
Jul 22, 2020·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Balasaheb D VanjareKi Hwan Lee
May 6, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Birutė Sapijanskaitė-BanevičVytautas Mickevičius

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