3845-20-3Relevant academic research and scientific papers
Chromene-containing aromatic sulfonamides with carbonic anhydrase inhibitory properties
Angeli, Andrea,Kartsev, Victor,Petrou, Anthi,Pinteala, Mariana,Brovarets, Volodymyr,Slyvchuk, Sergii,Pilyo, Stepan,Geronikaki, Athina,Supuran, Claudiu T.
, (2021/05/19)
Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological conditions. A series of chromene-based sulfonamides were synthesized and tested as possible CA inhibitors. Their inhibitory activity was assessed against the cytosolic human isoforms hCA I, hCA II and the transmembrane hCA IX and XII. Several of the investigated derivatives showed interesting inhibition activity towards the tumor associate isoforms hCA IX and hCA XII. Furthermore, computational procedures were used to investigate the binding mode of this class of compounds, within the active site of hCA IX.
Carbonic anhydrase inhibition with sulfonamides incorporating pyrazole-and pyridazinecarboxamide moieties provides examples of isoform-selective inhibitors
Angeli, Andrea,Brovarets, Volodymyr,Geronikaki, Athina,Kartsev, Victor,Panchishin, Svitlana,Petrou, Anthi,Pinteala, Mariana,Supuran, Claudiu T.,Vydzhak, Roman
, (2021/11/30)
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 ob-served 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.
