Carta, F. and Innocenti, A. and Hall, R.A. and Muhlschlegel, F.A. and Scozzafava, A. and Supuran, C.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.
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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: | 27 Jun 2012 09:49 |
| Resource URI: | http://kar.kent.ac.uk/id/eprint/29004 (The current URI for this page, for reference purposes) |
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