期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 17, 页码 5168-5174出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.06.035
关键词
Human carbonic anhydrase inhibitors; Benzenesulfonamide; 4,5,6,7-Tetrachloro-1,3-dioxoisoindolin-2-yl benzenesulfonamide; Structure-activity relationship
资金
- EU
A series of 4,5,6,7-tetrachloro-1,3-dioxoisoindolin-2-yl benzenesulfonamide derivatives (compounds 1-8) was synthesized by reaction of benzene sulfonamides incorporating primary amino moieties with 4,5,6,7-tetrachlorophthalic anhydride. These sulfonamides were assayed as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Some of these compounds showed very good in vitro human carbonic anhydrase (hCA) isoforms I, II and VII inhibitory properties, with affinities in the low nanomolar range. Inhibition activities against hCA I were in the range of 159-444 nM; against hCA II in the range of 2.4-4515 nM, and against hCA VII in the range of 1.3-469 nM. The structure-activity relationship (SAR) with this series of sulfonamides is straightforward, with the main features leading to good activity for each isoform being established. (C) 2013 Elsevier Ltd. All rights reserved.
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