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Carbonic anhydrase inhibitors. Inhibition of the fungal β-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids

Innocenti, Alessio, Winum, Jean-Yves, Hall, Rebecca A., Mühlschlegel, Fritz A., Scozzafava, Andrea, Supuran, Claudiu T. (2009) Carbonic anhydrase inhibitors. Inhibition of the fungal β-carbonic anhydrases from Candida albicans and Cryptococcus neoformans with boronic acids. Bioorganic & Medicinal Chemistry Letters, 19 (10). pp. 2642-2645. ISSN 0960-894X. (doi:10.1016/j.bmcl.2009.03.147) (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) (KAR id:91846)

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.
Official URL
https://doi.org/10.1016/j.bmcl.2009.03.147

Abstract

Inhibition of the beta-carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic fungi Cryptococcus neoformans (Can2) and Candida albicans (Nce103) with a series of aromatic, arylalkenyl- and arylalkylboronic acids was investigated. Aromatic, 4-phenylsubstituted- and 2-naphthylboronic acids were the best Can2 inhibitors, with inhibition constants in the range of 8.5-11.5microM, whereas arylalkenyl and aryalkylboronic acids showed K(I)s in the range of 428-3040microM. Nce103 showed a similar inhibition profile, with the 4-phenylsubstituted- and 2-naphthylboronic acids possessing K(I)s in the range of 7.8-42.3microM, whereas the arylalkenyl and aryalkylboronic acids were weaker inhibitors (K(I)s of 412-5210microM). The host human enzymes CA I and II were also effectively inhibited by these boronic acids. The B(OH)(2) moiety is thus a new zinc-binding group for designing effective inhibitors of the alpha- and beta-CAs.

Item Type: Article
DOI/Identification number: 10.1016/j.bmcl.2009.03.147
Divisions: Divisions > Division of Natural Sciences > Biosciences
Depositing User: Becky Hall
Date Deposited: 01 Dec 2021 09:39 UTC
Last Modified: 02 Dec 2021 22:39 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/91846 (The current URI for this page, for reference purposes)
Hall, Rebecca A.: https://orcid.org/0000-0002-4908-8168
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