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Issue 70, 2012
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Hydroxamate represents a versatile zinc binding group for the development of new carbonic anhydrase inhibitors

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Abstract

Hydroxamates (R–CONHOH) have been scarcely investigated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs). An inhibition/structural study of PhCONHOH is reported against all human isoforms. Comparing aliphatic (R = Me and CF3) and aromatic (R = Ph) hydroxamates as CAIs, we prove that CONHOH is a versatile zinc binding group. Depending on the nature of the R moiety, it can adopt different coordination modes to the catalytic ion within the CA active site.

Graphical abstract: Hydroxamate represents a versatile zinc binding group for the development of new carbonic anhydrase inhibitors

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Publication details

The article was received on 14 Jun 2012, accepted on 16 Jul 2012 and first published on 17 Jul 2012


Article type: Communication
DOI: 10.1039/C2CC34275H
Citation: Chem. Commun., 2012,48, 8838-8840
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    Hydroxamate represents a versatile zinc binding group for the development of new carbonic anhydrase inhibitors

    A. Di Fiore, A. Maresca, C. T. Supuran and G. De Simone, Chem. Commun., 2012, 48, 8838
    DOI: 10.1039/C2CC34275H

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