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Bioorg Med Chem Lett. 2015 Aug 15;25(16):3281-4. doi: 10.1016/j.bmcl.2015.05.076. Epub 2015 May 30.

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 information

1
Department of Life and Environmental Sciences, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.
2
Department of Life and Environmental Sciences, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy. Electronic address: maccione@unica.it.
3
Dipartimento di Scienze della Salute, Università Magna Graecia di Catanzaro, Campus 'S. Venuta', Viale Europa, 88100 Catanzaro, Italy.
4
Dipartimento NEUROFARBA, Sezione di Scienze Farmaceutiche, Università degli Studi di Firenze, Sesto Fiorentino, Florence, Italy.

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.

KEYWORDS:

Carbonic anhydrase; Selective inhibitor; Sulfonamide; Tumor-associated isoform

PMID:
26073006
DOI:
10.1016/j.bmcl.2015.05.076
[Indexed for MEDLINE]

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