期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 23, 期 10, 页码 2598-2605出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.12.054
关键词
Sulfonamide; Imide; N-Acylsulfonamide; Carbonic anhydrase; Enzyme purification; Enzyme inhibition
资金
- Ataturk University [TUBITAK 110T483]
- Research Chairs Program at King Saud University
Sulfonamides represent a significant class of biologically active compounds that inhibit carbonic anhydrase (CA, EC.: 4.2.1.1) isoenzymes involved in different pathological and physiological events. Sulfonamide CA inhibitors are used therapeutically as diuretic, antiglaucoma, antiobesity and anticancer agents. A series of new sulfonamides were synthesized using imides and tosyl chloride as starting materials. These N-acylsulfonamides efficiently inhibited the cytosolic human carbonic anhydrase isoenzymes I, and II (hCA I, and II), with nanomolar range inhibition constants ranging between 36.4 +/- 6.0-254.6 +/- 18.0 and 58.3 +/- 0.6-273.3 +/- 2.5 nM, respectively. (C) 2015 Elsevier Ltd. All rights reserved.
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