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Carbonic Anhydrase Inhibition with Sulfonamides Incorporating Pyrazole- and Pyridazinecarboxamide Moieties Provides Examples of Isoform-Selective Inhibitors

Authors :
Svitlana Ya. Panchishin
Andrea Angeli
Anthi Petrou
Victor Kartsev
Athina Geronikaki
Mariana Pinteala
Claudiu T. Supuran
R. N. Vydzhak
Volodymyr Brovarets
Source :
Molecules, Vol 26, Iss 7023, p 7023 (2021), Molecules, Volume 26, Issue 22
Publication Year :
2021
Publisher :
MDPI AG, 2021.

Abstract

A series of benzenesulfonamides incorporating pyrazole- and pyridazinecarboxamides decorated with several bulky moieties has been obtained by original procedures. The new derivatives were investigated for the inhibition of four physiologically crucial human carbonic anhydrase (hCA, EC 4.2.2.1.1) isoforms, hCA I and II (cytosolic enzymes) as well as hCA IX and XII (transmembrane, tumor-associated isoforms). Examples of isoform-selective inhibitors were obtained for all four enzymes investigated here, and a computational approach was employed for explaining the observed selectivity, which may be useful in drug design approaches for obtaining inhibitors with pharmacological applications useful as antiglaucoma, diuretic, antitumor or anti-cerebral ischemia drugs.

Details

Language :
English
ISSN :
14203049
Volume :
26
Issue :
7023
Database :
OpenAIRE
Journal :
Molecules
Accession number :
edsair.doi.dedup.....7576457fd385a98d9a4a0b7803b5eadf