Bioorganic and Medicinal Chemistry Letters p. 3014 - 3018 (2017)
Update date:2022-08-11
Topics:
Mente?e, Emre
Bekta?, Hakan
Sokmen, Bahar Bilgin
Emirik, Mustafa
?ak?r, Demet
Kahveci, Bahittin
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?=?0.06?μM. Molecular docking studies were also conducted on enzyme extracted from Jack bean urease to identify the binding mode of the newly synthesized compounds.
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Doi:10.1021/acs.orglett.8b03057
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