Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives

Carta, Fabrizio and Innocenti, Alessio and Hall, Rebecca A. and Mühlschlegel, Fritz A. and Scozzafava, Andrea and Supuran, Claudiu T. (2011) Carbonic anhydrase inhibitors. Inhibition of the β-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with branched aliphatic/aromatic carboxylates and their derivatives. Bioorganic & Medicinal Chemistry Letters, 21 (8). pp. 2521-2526. ISSN 0960-894X. (The full text of this publication is not available from this repository)

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Official URL
http://dx.doi.org/10.1016/j.bmcl.2011.02.057

Abstract

The inhibition of the β-carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic fungi Cryptococcus neoformans (Can2) and Candida albicans (Nce103) with a series of 25 branched aliphatic and aromatic carboxylates has been investigated. Human isoforms hCA I and II were also included in the study for comparison. Aliphatic carboxylates were generally millimolar hCA I and II inhibitors and low micromolar/submicromolar β-CA inhibitors. Aromatic carboxylates were micromolar inhibitors of the four enzymes but some of them showed low nanomolar activity against the fungal pathogenic enzymes. 4-Hydroxy- and 4-methoxy-benzoate inhibited Can2 with K(I)s of 9.5-9.9 nM. The methyl esters, hydroxamates, hydrazides and carboxamides of some of these derivatives were also effective inhibitors of the α- and β-CAs investigated here.

Item Type: Article
Subjects: Q Science > Q Science (General)
Divisions: Faculties > Science Technology and Medical Studies > School of Biosciences > Biomedical Research Group
Depositing User: Sue Davies
Date Deposited: 08 Mar 2012 13:59
Last Modified: 09 Apr 2014 15:54
Resource URI: http://kar.kent.ac.uk/id/eprint/29004 (The current URI for this page, for reference purposes)
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