Carbonic anhydrase inhibitors: water-soluble 4-sulfamoylphenylthioureas as topical intraocular pressure-lowering agents with long-lasting effects

…, A Scozzafava, F Mincione, L Menabuoni…

Index: Casini; Scozzafava; Mincione; Menabuoni; Ilies; Supuran Journal of Medicinal Chemistry, 2000 , vol. 43, # 25 p. 4884 - 4892

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Citation Number: 122

Abstract

A series of sulfonamides has been obtained by reaction of 4- isothiocyanatobenzenesulfonamide with amines, amino acids, and oligopeptides. The new thiourea derivatives showed strong affinities toward isozymes I, II, and IV of carbonic anhydrase (CA, EC 4.2. 1.1). In vitro inhibitory power was good (in the low-nanomolar range) for the derivatives of β-phenylserine and α-phenylglycine, for those incorporating ...