Pharmaceutical Chemistry Section, Van Yüzüncü Yil University, Van, Turkey.
Department of Chemistry, Faculty of Sciences, Atatürk University, Erzurum, Turkey.
Arch Pharm (Weinheim). 2021 Oct;354(10):e2100188. doi: 10.1002/ardp.202100188. Epub 2021 Jun 7.
In this study, 23 different imidazole derivatives were synthesized, and the inhibitory properties of these derivatives against carbonic anhydrase I and II isoenzymes were investigated for the first time. The inhibition concentrations of the imidazole derivatives were found to be in the range of 2.89-115.5 nM. Docking studies examined the binding properties of the imidazole derivatives, and the structure-activity relationship is discussed. Theoretical calculations showed that the binding mode of the imidazole ring was non-zinc binding.
在这项研究中，合成了 23 种不同的咪唑衍生物，并首次研究了这些衍生物对碳酸酐酶 I 和 II 同工酶的抑制特性。咪唑衍生物的抑制浓度范围在 2.89-115.5 nM 之间。对接研究考察了咪唑衍生物的结合特性，并讨论了构效关系。理论计算表明，咪唑环的结合方式是非锌结合。
