期刊
ARCHIV DER PHARMAZIE
卷 347, 期 12, 页码 950-957出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201400257
关键词
Aminoindane; Aniline; Carbonic anhydrase; Enzyme inhibition; Sulfamide; Sulfamoyl carbamate
资金
- Scientific and Technological Research Council of Turkey (TUBITAK) [TBAG-109T241]
- Ataturk University [BAP2012/152, BAP 2013/284]
- Research Chairs Program at King Saud University
Three 1-aminoindanes, four anilines and BnOH or t-BuOH were reacted with chlorosulfonyl isocyanate to give sulfamoyl carbamates. Pd-C catalysed hydrogenolysis reactions of carbamates or deprotection of the Boc group of the carbamates with CF3CO2H afforded seven novel sulfamides. Human carbonic anhydrase (hCA) isoenzymes I and II (hCA I and hCA II) were purified from fresh human blood erythrocytes with one-step affinity chromatography on Sepharose 4B-tyrosine-sulfanilamide. The inhibitory properties of the novel sulfamides on both isoenzymes were determined using the esterase activity with 4-nitrophenyl acetate (NPA) as substrate. The tested novel sulfamides derived from 1-aminoindanes and anilines effectively inhibited hCA I and II competitively in the nanomolar range. Among these compounds, the novel sulfamide derivative 17 showed the most potent inhibitory effect against hCA I (K-i: 153.88 nM), while sulfamide derivative 26 showed the highest inhibitory potential against hCA II (K-i: 117.80 nM).
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。
推荐
暂无数据