Sulfonamides incorporating heteropolycyclic scaffolds show potent inhibitory action against carbonic anhydrase isoforms I, II, IX and XII

Bioorganic & Medicinal Chemistry
Elisabetta BarresiClaudiu T Supuran

Abstract

Three series of polycyclic compounds possessing either primary sulfonamide or carboxylic acid moieties as zinc-binding groups were investigated as inhibitors of four physiologically relevant CA isoforms, the cytosolic hCA I and II, as well as the transmembrane hCA IX and XII. Most of the new sulfonamides reported here showed excellent inhibitory effects against isoforms hCA II, IX and XII, but no highly isoform-selective inhibition profiles. On the other hand, the carboxylates selectively inhibited hCA IX (KIs ranging between 40.8 and 92.7nM) without inhibiting significantly the other isoforms. Sulfonamides/carboxylates incorporating polycyclic ring systems such as benzothiopyranopyrimidine, pyridothiopyranopyrimidine or dihydrobenzothiopyrano[4,3-c]pyrazole may be considered as interesting candidates for exploring the design of isoform-selective CAIs with various pharmacologic applications.

References

Jan 3, 2008·Nature Reviews. Drug Discovery·Claudiu T Supuran
Dec 8, 2011·Journal of Enzyme Inhibition and Medicinal Chemistry·Ramazan DemirdağClaudiu T Supuran
Apr 4, 2012·Journal of Enzyme Inhibition and Medicinal Chemistry·Claudiu T Supuran
Jan 17, 2013·Journal of Enzyme Inhibition and Medicinal Chemistry·Sonia Del PreteClemente Capasso
Feb 6, 2013·Journal of Enzyme Inhibition and Medicinal Chemistry·Claudiu T Supuran
Feb 16, 2013·Journal of Enzyme Inhibition and Medicinal Chemistry·Fortunato MigliardiniClemente Capasso
May 1, 2013·Journal of Enzyme Inhibition and Medicinal Chemistry·Clemente Capasso, Claudiu T Supuran
Aug 7, 2013·Journal of Enzyme Inhibition and Medicinal Chemistry·Sonia Del PreteClemente Capasso
Jan 25, 2014·Journal of Enzyme Inhibition and Medicinal Chemistry·Sonia Del PreteClemente Capasso
Dec 2, 2015·Journal of Enzyme Inhibition and Medicinal Chemistry·Claudiu T Supuran

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Citations

Sep 1, 2016·Journal of Enzyme Inhibition and Medicinal Chemistry·Kaan KucukogluHalise Inci Gul
Oct 27, 2016·Expert Opinion on Drug Discovery·Claudiu T Supuran

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