Chromone containing sulfonamides as potent carbonic anhydrase inhibitors

被引:45
作者
Ekinci, Deniz [2 ]
al-Rashida, Mariya [3 ]
Abbas, Ghulam [3 ]
Senturk, Murat [1 ]
Supuran, Claudiu T. [4 ]
机构
[1] Ibrahim Cecen Univ Agri, Sci & Art Fac, Dept Chem, Agri, Turkey
[2] Ondokuz Mayis Univ, Fac Agr, Dept Agr Biotechnol, Samsun, Turkey
[3] Univ Punjab, Inst Chem, Lahore, Pakistan
[4] Univ Florence, Lab Chim Bioinorgan, Florence, Italy
关键词
Human carbonic anhydrase; enzyme inhibitors; sulfonamides; schiff's base; IN-VITRO INHIBITION; THERAPEUTIC APPLICATIONS; PHENOLIC-COMPOUNDS; ISOZYME-II; X-RAY; BINDING; AGENTS; ACTIVATORS;
D O I
10.3109/14756366.2011.614607
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
摘要
A series of sulfonamide derivatives incorporating substituted 3-formylchromone moieties were investigated for the inhibition of three human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, hCA I, II, and VI. All these compounds, together with the clinically used sulfonamide acetazolamide, were investigated as inhibitors of the physiologically relevant isozymes I, II (cytosolic), and VI (secreted isoform). These sulfonamides showed effective inhibition against all these isoforms with K's in the range of 0.228 to 118 mu M. Such molecules can be used as leads for discovery of novel effective CA inhibitors against other isoforms with medicinal chemistry applications.
引用
收藏
页码:744 / 747
页数:4
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