Menteşe Emre, Bektaş Hakan, Sokmen Bahar Bilgin, Emirik Mustafa, Çakır Demet, Kahveci Bahittin
Department of Chemistry, Art and Science Faculty, Recep Tayyip Erdogan University, Rize, Turkey.
Department of Chemistry, Faculty of Arts and Sciences, Giresun University, 28049 Giresun, Turkey.
Bioorg Med Chem Lett. 2017 Jul 1;27(13):3014-3018. doi: 10.1016/j.bmcl.2017.05.019. Epub 2017 May 10.
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 IC=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.
以5,6-二氯-2-环丙基-1H-苯并咪唑为起始原料，合成了一系列包含肼基甲硫酰胺、1,2,4-三唑、1,3,4-恶二唑和亚胺官能团的新型苯并咪唑化合物。所有苯并咪唑衍生物均表现出良好的脲酶抑制活性。化合物6a被证明是最有效的，其酶抑制活性的IC=0.06µM。还对刀豆脲酶提取的酶进行了分子对接研究，以确定新合成化合物的结合模式。
