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)
The inhibition of the β-carbonic anhydrases (CAs, EC 22.214.171.124) 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.
|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:||22 Apr 2014 14:39|
|Resource URI:||http://kar.kent.ac.uk/id/eprint/29004 (The current URI for this page, for reference purposes)|