A novel series of hydantoins incorporating phthalimides has been synthesised by condensation of activated phthalimides with 1-aminohydantoin and investigated for their inhibitory activity against a panel of human (h) carbonic anhydrase (CA, EC 4.2.1.1): the cytosolic isoforms hCA I, hCA II, and hCA VII, secreted isoform hCA VI, and the transmembrane hCA IX, by a stopped-flow CO hydrase assay. Although all newly developed compounds were totally inactive on hCA I and mainly ineffective towards hCA II, they generally exhibited moderate repressing effects on hCA VI, VII, and IX with s values in the submicromolar to micromolar ranges. The salts and , followed by derivative , displayed the best inhibitory activity of all the evaluated compounds and their binding mode was proposed . These compounds can also be considered interesting starting points for the development of novel pharmacophores for this class of enzyme inhibitors.
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| http://dx.doi.org/10.1080/14756366.2024.2335927 | DOI Listing |
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