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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
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SYSNO ASEP 0343450 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Identification of 3,4-Dihydroisoquinoline-2(1H)-sulfonamides as Potent Carbonic AnhydraseInhibitors: Synthesis, Biological Evaluation, and Enzyme-Ligand X-ray Studies Author(s) Gitto, R. (IT)
Agnello, S. (IT)
Ferro, S. (IT)
De Luca, L. (IT)
Vullo, D. (IT)
Brynda, Jiří (UOCHB-X) RID, ORCID
Mader, Pavel (UMG-J)
Supuran, C. T. (IT)
Chimirri, A. (IT)Number of authors 9 Source Title Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 53, č. 6 (2010), s. 2401-2408Number of pages 8 s. Language eng - English Country US - United States Keywords inhibitor design ; crystal structure ; X-ray analysis ; dehalogenase Subject RIV CC - Organic Chemistry R&D Projects GA203/09/0820 GA ČR - Czech Science Foundation (CSF) CEZ AV0Z40550506 - UOCHB-X (2005-2011) AV0Z50520514 - UMG-J (2005-2011) UT WOS 000275711000008 DOI 10.1021/jm9014026 Annotation 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Year of Publishing 2011
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