A series of new thienyl-substituted pyrazoline benzenesulfonamides were synthesized and their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were tested on the human (h) isoforms hCA I and hCA II. The inhibition constant (Ki) of these sulfonamides were in the range of 232.16-637.70 nM toward the slow cytosolic isozyme hCA I, and in the range of 342.07-455.80 nM toward hCA II. Many of these compounds showed comparable inhibition with the reference sulfonamide acetazolamide, a clinically used drug. As the sulfonamide CA inhibitors (CAIs) show many therapeutic uses, these derivatives represent interesting examples of a novel class of such derivatives.
Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides / Mete, Ebru; Comez, Birnur; Inci Gul, Halise; Gulcin, Ilhami; Supuran, Claudiu T.. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - STAMPA. - 31:(2016), pp. 1-5. [10.1080/14756366.2016.1181627]
Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides
SUPURAN, CLAUDIU TRANDAFIR
2016
Abstract
A series of new thienyl-substituted pyrazoline benzenesulfonamides were synthesized and their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were tested on the human (h) isoforms hCA I and hCA II. The inhibition constant (Ki) of these sulfonamides were in the range of 232.16-637.70 nM toward the slow cytosolic isozyme hCA I, and in the range of 342.07-455.80 nM toward hCA II. Many of these compounds showed comparable inhibition with the reference sulfonamide acetazolamide, a clinically used drug. As the sulfonamide CA inhibitors (CAIs) show many therapeutic uses, these derivatives represent interesting examples of a novel class of such derivatives.I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.