4.6 Article

Synthesis, characterization, carbonic anhydrase inhibitor activity, and docking studies of phenylthiazol-2 (3h)-ylidene-isoquinoline-5-amine Derivatives

期刊

JOURNAL OF MOLECULAR STRUCTURE
卷 1291, 期 -, 页码 -

出版社

ELSEVIER
DOI: 10.1016/j.molstruc.2023.136061

关键词

Isoquinoline; Thiazole; Thiourea; Carbonic anhydrase; Enzyme inhibitor

向作者/读者索取更多资源

Phenylthiazol-2(3h)-ylidene-isoquinoline-5-amine derivatives (5a-r) were easily synthesized using a two-step method from 5-aminoisoquinoline, thioisocyanate, and phenacyl bromide derivatives. The newly synthesized compounds were characterized using 1H NMR, 13C NMR, IR, and elemental analysis. Their inhibitory effects on hydratase and esterase activities of carbonic anhydrase isoenzymes (hCA I, II, IX, and X) were studied in vitro.
Phenylthiazol-2(3h)-ylidene-isoquinoline-5-amine derivatives(5a-r) were easily prepared from 5-aminoisoquinoline, thioisocyanate, and phenacyl bromide derivatives in the presence of triethylamine in tetrahydrofuran (THF), and dimethyl formamide (DMF) in two steps. In the first step, thiourea was synthesized in THF reflux, 24 h and then in the second step, the formation of thiazole ring was ensured in EtOH-DMF (5:5 v/v), reflux, 24 h. The newly synthesized compounds were characterized using 1H NMR, 13C NMR, IR, and elemental analysis. The inhibitory effects of 18 newly synthesized compounds (5a-r) on hydratase and esterase activities of carbonic anhydrase isoenzymes (hCA I, II, IX, and X) were studied in vitro.

作者

我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。

评论

主要评分

4.6
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据