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

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info:eu-repo/semantics/closedAccess

Date

2017

Author

Mentese, Emre
Bektas, Hakan
Sokmen, Bahar Bilgin
Emirik, Mustafa
Cakir, Demet
Kahveci, Bahittin

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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 = 0.06 mu M. Molecular docking studies were also conducted on enzyme extracted from Jack bean urease to identify the binding mode of the newly synthesized compounds. (C) 2017 Elsevier Ltd. All rights reserved.

Source

Bioorganic & Medicinal Chemistry Letters

Volume

27

Issue

13

URI

https://doi.org/10.1016/j.bmcl.2017.05.019
https://hdl.handle.net/11436/2101

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  • PubMed İndeksli Yayınlar Koleksiyonu [1026]
  • Scopus İndeksli Yayınlar Koleksiyonu [3485]
  • WoS İndeksli Yayınlar Koleksiyonu [2792]



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