Synthesis and evaluation of sulfonamide-bearing thiazole as carbonic anhydrase isoforms hCA I and hCA II

被引：28

作者：

Kilicaslan, Soner ^{[1
]}

Arslan, Mustafa ^{[1
]}

Ruya, Zeynep ^{[1
]}

Bilen, Cigdem ^{[2
]}

Ergun, Adem ^{[2
]}

Gencer, Nahit ^{[2
]}

Arslan, Oktay ^{[2
]}

机构：

[1] Sakarya Univ, Fac Arts & Sci, Dept Chem, Sakarya, Turkey

[2] Balikesir Univ, Fac Arts & Sci, Dept Chem, TR-10145 Balikesir, Turkey

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2016年 / 31卷 / 06期

关键词：

Carbonic anhydrase; enzyme inhibitor; sulfonamide; thiazole; INHIBITORY PROPERTIES; CYANAMIDE HYDRATION; ESTERASE-ACTIVITIES; VITRO INHIBITION; DERIVATIVES; MECHANISM; ISOZYMES; COUMARINS; DRUGS;

D O I：

10.3109/14756366.2015.1128426

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Sulfonamide-bearing thiazole compounds were synthesized and their inhibitory effects on the activity of purified human carbonic anhydrase I and II were evaluated. Human carbonic anhydrase isoenzymes (hCA-I and hCA-II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of the 12 synthesized sulfonamide (5a-l) on the hydratase and esterase activities of these isoenzymes (hCA-I and hCA-II) were studied in vitro. In relation to these activities, the inhibition equilibrium constants (Ki) were determined. The results showed that all the synthesized compounds inhibited the CA isoenzyme activity. Among them 5b was found to be the most active (IC50 = 0.35 mu M; Ki: 0.33 mu M) for hCA I and hCA II.

引用

页码：1300 / 1305

页数：6

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