Hydroxamate represents a versatile zinc binding group for the development of new carbonic anhydrase inhibitors |
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Authors: | Anna Di Fiore Alfonso Maresca Claudiu T Supuran Giuseppina De Simone |
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Institution: | Istituto di Biostrutture e Bioimmagini - CNR, Napoli, Italy. gdesimon@unina.it. |
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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 CF(3)) 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. |
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