A series of novel 1,3-thiazole sulfonamides 7a-7o have been designed, synthesized and studied their CA inhibitory properties. The inhibition property of four human CA isoforms was investigated: hCA I, II, IX, and XII using the standard drug acetazolamide (AAZ) for comparison. Compounds 7a-7o showed a wide range of inhibiton potency towards the cytosolic enzyme hCA I. Nevertheless, 7a, 7c, 7i/7j and 7m molecules have shown higher inhibition potential as compared to Acetazolamide (KI = 250 nM). Finally, the second tumor membrane-associated isoform, hCA XII showed a wide range of potency that spanned from 9.3 to 729.6 nM. These compounds have the potential to show antibacterial, antifungal, antiretroviral, and other biological activities and thus can direct the studies in the field of pharmaceuticals of new drug design.
Design, synthesis and human carbonic anhydrase I, II, IX and XII inhibitory properties of 1,3-thiazole sulfonamides / Erigur E.C.; Altug C.; Angeli A.; Supuran C.T.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - ELETTRONICO. - 59:(2022), pp. 128581.128581-128581.128581. [10.1016/j.bmcl.2022.128581]
Design, synthesis and human carbonic anhydrase I, II, IX and XII inhibitory properties of 1,3-thiazole sulfonamides
Angeli A.;Supuran C. T.
2022
Abstract
A series of novel 1,3-thiazole sulfonamides 7a-7o have been designed, synthesized and studied their CA inhibitory properties. The inhibition property of four human CA isoforms was investigated: hCA I, II, IX, and XII using the standard drug acetazolamide (AAZ) for comparison. Compounds 7a-7o showed a wide range of inhibiton potency towards the cytosolic enzyme hCA I. Nevertheless, 7a, 7c, 7i/7j and 7m molecules have shown higher inhibition potential as compared to Acetazolamide (KI = 250 nM). Finally, the second tumor membrane-associated isoform, hCA XII showed a wide range of potency that spanned from 9.3 to 729.6 nM. These compounds have the potential to show antibacterial, antifungal, antiretroviral, and other biological activities and thus can direct the studies in the field of pharmaceuticals of new drug design.
I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
