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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.
- 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.)
- 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
Subjects
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