期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 27, 期 5, 页码 744-747出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2011.614607
关键词
Human carbonic anhydrase; enzyme inhibitors; sulfonamides; schiff's base
资金
- Turkish Republic Prime Ministry State Planning Organization (DPT) [2010K120440]
- Agri Ibrahim Cecen University Scientific Research Council [Agri BAP-2010/K-10]
- EU
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.
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