Thia- and Seleno-Michael Reactions for the Synthesis of Carbonic Anhydrases Inhibitors

Novel chalcogen-containing amides and esters bearing the benzenesulfonamide moiety have been synthesised upon nucleophilic conjugate addition of thiols and selenols to suitable electron-deficient alkenes. The activity of the synthesised compounds as Carbonic Anhydrases inhibitors has been investigated in vitro and the inhibition mechanism has been elucidated by X-rays studies.A series of chalcogen-containing carbonic anhydrase inhibitors have been synthesised via nucleophilic conjugate addition of thiols and selenols to electron-deficient alkenes bearing the benzenesulfonamide moiety. The activity of the synthesised compounds has been investigated in vitro and the inhibition mechanism has been elucidated by X-rays studies. image