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. Issue 16 (15th August 2015)

• Record Type: Journal Article
• Authors: Meleddu, Rita; Maccioni, Elias; Distinto, Simona; Bianco, Giulia; Melis, Claudia; Alcaro, Stefano; Cottiglia, Filippo; Ceruso, Mariangela; Supuran, Claudiu T.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 16(2015)
• Page Start: 3281
• Page End: 3284
• Publication Date: 2015-08-15
• Subjects: KBYGAQLHLOBGDS-CYGOZCHUSA-N; Carbonic anhydrase -- Sulfonamide -- Tumor-associated isoform -- Selective inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.05.076
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical 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.