期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 30, 期 5, 页码 737-745出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2014.963072
关键词
Carbonic anhydrase; fluorine; selectivity; superacid; tertiary benzenesulfonamides
资金
- Universite de Poitiers
- CNRS
- @rtMolecule
- ANRT (CIFRE scholarship)
- EU
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.
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