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

Carta, Fabrizio, Innocenti, Alessio, Hall, Rebecca A., Mühlschlegel, Fritz A., Scozzafava, Andrea, Supuran, Claudiu T. (2011) Carbonic anhydrase inhibitors. Inhibition of the ?-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. (doi:10.1016/j.bmcl.2011.02.057) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided. (Contact us about this Publication)
Official URL
http://dx.doi.org/10.1016/j.bmcl.2011.02.057

Abstract

The inhibition of the ?-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 ?-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 ?- and ?-CAs investigated here.

Item Type: Article
DOI/Identification number: 10.1016/j.bmcl.2011.02.057
Subjects: Q Science > Q Science (General)
Divisions: Faculties > Sciences > School of Biosciences > Biomedical Research Group
Depositing User: Sue Davies
Date Deposited: 08 Mar 2012 13:59 UTC
Last Modified: 29 May 2019 08:52 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/29004 (The current URI for this page, for reference purposes)
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