New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII

MELEDDU, RITA;MACCIONI, ELIAS;DISTINTO, SIMONA;BIANCO, GIULIA;MELIS, CLAUDIA;COTTIGLIA, FILIPPO;
2015-01-01

Abstract

Abstract A series of 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides was synthesised and the activity of the new compounds as inhibitors of hCA I, II, IX, and XII was evaluated. These new derivatives exhibited some peculiarities with respect to previously reported sulfonamide based inhibitors of CA. We observed that the nature of the substituents in the position 3 and 4 of the dihydro-thiazole ring was relevant in determining both activity and selectivity profiles.
2015
Carbonic anhydrase; Selective inhibitor; Sulfonamide; Tumor-associated isoform; Binding sites; Carbonic anhydrase I; Carbonic anhydrase II; Carbonic anhydrase inhibitors; Carbonic anhydrases; Enzyme activation; Humans; Isoenzymes; Models, biological; Molecular structure; Sulfonamides; Thiazoles; Triazoles; Biochemistry; Clinical biochemistry; Molecular biology; Molecular medicine; Organic chemistry; Drug discovery; Pharmaceutical science; Medicine (all)
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