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

…, A Scozzafava, F Mincione, L Menabuoni…

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

全文：HTML全文

被引用次数: 122

摘要

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 ...