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

作者：Di Fiore Anna; Maresca Alfonso; Supuran Claudiu T^*; De Simone Giuseppina

来源：Chemical communications, 2012, 48(70): 8838-8840.

DOI：10.1039/c2cc34275h

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.

• 出版日期2012