期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 10, 页码 2867-2874出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.03.041
关键词
Carbonic anhydrase; Inhibitor; Sulfonamide; Schiff's base; Amine; Imine
资金
- ITN Marie Curie Network-DYNANO [PITN-GA-2011-289033]
A library of Schiff bases was synthesized by condensation of aromatic amines incorporating sulfonamide, carboxylic acid or carboxymethyl functionalities as Zn2+-binding groups, with aromatic aldehydes incorporating tert-butyl, hydroxy and/or methoxy groups. The corresponding amines were thereafter obtained by reduction of the imines. These compounds were assayed for the inhibition of two cytosolic human carbonic anhydrase (hCA, EC 4.2.1.1) isoenzymes, hCA I and II. The K-i values of the Schiff bases were in the range of 7.0-21,400 nM against hCA II and of 52-8600 nM against hCA I, respectively. The corresponding amines showed Ki values in the range of 8.6 nM-5.3 mu M against hCA II, and of 18.7-251 nM against hCA I, respectively. Unlike the imines, the reduced Schiff bases are stable to hydrolysis and several low-nanomolar inhibitors were detected, most of them incorporating sulfonamide groups. Some carboxylates also showed interesting CA inhibitory properties. Such hydrosoluble derivatives may show pharmacologic applications. (C) 2014 Elsevier Ltd. All rights reserved.
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