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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.

Authors :
Meleddu R
Maccioni E
Distinto S
Bianco G
Melis C
Alcaro S
Cottiglia F
Ceruso M
Supuran CT
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Aug 15; Vol. 25 (16), pp. 3281-4. Date of Electronic Publication: 2015 May 30.
Publication Year :
2015

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.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
25
Issue :
16
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
26073006
Full Text :
https://doi.org/10.1016/j.bmcl.2015.05.076