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
Thia- and Seleno-Michael Reactions for the Synthesis of Carbonic Anhydrases Inhibitors / Angeli A.; Occhini A.; Renzi G.; Capperucci A.; Ferraroni M.; Tanini D.; Supuran C.T.. - In: CHEMMEDCHEM. - ISSN 1860-7187. - ELETTRONICO. - (2024), pp. 0-0. [10.1002/cmdc.202400345]
Thia- and Seleno-Michael Reactions for the Synthesis of Carbonic Anhydrases Inhibitors
Angeli A.;Occhini A.;Renzi G.;Capperucci A.;Ferraroni M.;Tanini D.;Supuran C. T.
2024
Abstract
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
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