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Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as Potent Carbonic AnhydraseInhibitors: Synthesis, Biological Evaluation, and Enzyme-Ligand X-ray Studies
- 1.0343450 - ÚOCHB 2011 RIV US eng J - Journal Article
Gitto, R. - Agnello, S. - Ferro, S. - De Luca, L. - Vullo, D. - Brynda, Jiří - Mader, Pavel - Supuran, C. T. - Chimirri, A.
Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as Potent Carbonic AnhydraseInhibitors: Synthesis, Biological Evaluation, and Enzyme-Ligand X-ray Studies.
Journal of Medicinal Chemistry. Roč. 53, č. 6 (2010), s. 2401-2408. ISSN 0022-2623. E-ISSN 1520-4804
R&D Projects: GA ČR GA203/09/0820
Institutional research plan: CEZ:AV0Z40550506; CEZ:AV0Z50520514
Keywords : inhibitor design * crystal structure * X-ray analysis * dehalogenase
Subject RIV: CC - Organic Chemistry
Impact factor: 5.207, year: 2010
This work explores inhibitory effects a small class of 1-(cyclo)alkylisoquinolines containing a sulfonamide function on the activity of carbonic anhydrase (CA, EC 4.2.1.1). Some derivatives showed potent hCA IX and hCA XIV inhibitory effects at nanomolar concentrations as well as low affinity for the ubiquitous hCA II. We also report the X-ray crystal structure of one of these derivatives in complex with dominant human isoform II.
Permanent Link: http://hdl.handle.net/11104/0185928
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