Please use this identifier to cite or link to this item: https://hdl.handle.net/1959.11/22916
Title: Inhibition of human mitochondrial carbonic anhydrases VA and VB with para-(4-phenyltriazole-1-yl)-benzenesulfonamide derivatives
Contributor(s): Poulsen, Sally-Ann (author); Wilkinson, Brendan (author)orcid ; Innocenti, Alessio (author); Vullo, Daniela (author); Supuran, Claudiu T (author)
Publication Date: 2008
DOI: 10.1016/j.bmcl.2008.07.010
Handle Link: https://hdl.handle.net/1959.11/22916
Abstract: A library of 10 novel benzenesulfonamides containing triazole-tethered phenyl 'tail' moieties were synthesized by a Cu(I) catalyzed 1,3-dipolar cycloaddition reaction (DCR) (i.e., click chemistry) between 4-azido benzenesulfonamide and a panel of variously substituted phenyl acetylenes. These compounds were very effective inhibitors (low nanomolar) of the human mitochondrial carbonic anhydrase isozymes VA and VB. Mitochondrial carbonic anhydrases are potential targets for anti-obesity therapies, acting to reduce lipogenesis through a novel mechanism of action. The inhibitors reported here should prove valuable as lead compounds to further investigate the potential of CA inhibition for this novel therapeutic application.
Publication Type: Journal Article
Source of Publication: Bioorganic & Medicinal Chemistry Letters, 18(16), p. 4624-4627
Publisher: Pergamon Press
Place of Publication: United Kingdom
ISSN: 0960-894X
1464-3405
Field of Research (FOR): 030503 Organic Chemical Synthesis
030401 Biologically Active Molecules
030499 Medicinal and Biomolecular Chemistry not elsewhere classified
Peer Reviewed: Yes
HERDC Category Description: C1 Refereed Article in a Scholarly Journal
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Appears in Collections:Journal Article
School of Science and Technology

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