1. 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.
- Author
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Meleddu R, Maccioni E, Distinto S, Bianco G, Melis C, Alcaro S, Cottiglia F, Ceruso M, and Supuran CT
- Subjects
- Binding Sites, Carbonic Anhydrase Inhibitors chemical synthesis, Carbonic Anhydrase Inhibitors chemistry, Carbonic Anhydrase Inhibitors pharmacology, Enzyme Activation drug effects, Humans, Isoenzymes chemical synthesis, Isoenzymes chemistry, Isoenzymes pharmacology, Models, Biological, Molecular Structure, Sulfonamides chemistry, Thiazoles chemistry, Thiazoles pharmacology, Triazoles chemical synthesis, Triazoles chemistry, Triazoles pharmacology, Benzenesulfonamides, Carbonic Anhydrase I antagonists & inhibitors, Carbonic Anhydrase II antagonists & inhibitors, Carbonic Anhydrases metabolism, Sulfonamides chemical synthesis, Sulfonamides pharmacology, Thiazoles chemical synthesis
- 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., (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Published
- 2015
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