Fluorinated pyrrolidines and piperidines incorporating tertiary benzenesulfonamide moieties are selective carbonic anhydrase II inhibitors. (October 2015)

• Record Type: Journal Article
• Authors: Le Darz, Alexandre; Mingot, Agnès; Bouazza, Fodil; Castelli, Ugo; Karam, Omar; Tanc, Muhammet; Supuran, Claudiu T.; Thibaudeau, Sébastien
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 30:Number 5(2015:Oct.)
• Page Start: 737
• Page End: 745
• Publication Date: 2015-10
• Subjects: Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• Languages: English
• ISSNs: 1475-6366

Abstract

<abstract> <title>Abstract</title> <p>A series of substituted pyrrolidines and piperidines were synthesized using superacid HF/SbF₅ chemistry. Investigated as inhibitors of several human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, i.e. the cytosolic hCA I and II as well as the tumor-associated transmembrane isoforms hCA IX and XII, these compounds showed a never yet reported selectivity toward the human carbonic anhydrase hCA II. In the tertiary benzenesulfonamide family, this class of inhibitors points out a new mechanism of action for human carbonic anhydrase II inhibition.</p> </abstract>