Synthesis and structure–activity relationships of novel benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II

This manuscript reports the identification of a novel series of mono- and bis- benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II (bCAII). These compounds exhibited nanomolar equilibrium dissociation constants with Ki’s ranging from 4.7 to 9.3 nM. All compounds were ester derivatives of the weak affinity bCAII inhibitor, 4-carboxybenzenesulfonamide. Structure–activity relationships for this novel series of compounds are discussed.

The synthesis and structure–activity relationships of a novel series of mono- and bis- benzene sulfonamides with potent binding affinity for bovine carbonic anhydrase II are reported.Figure optionsDownload as PowerPoint slide