advertisement
Abstract #9931 Published in IGR 5-3
Carbonic anhydrase inhibitors: topically acting antiglaucoma sulfonamides incorporating esters and amides of 3- and 4-carboxybenzolamide
Casini A; Scozzafava A; Mincione F; Menabuoni L; Starnotti M; Supuran CTBioorganic and Medicinal Chemistry Letters 2003; 13: 2867-2873
Reaction of 3- and 4-carboxybenzenesulfonyl chloride with 5-amino-1,3,4-thiadiazole-2-sulfonamide/5-imino-4-methyl-δ2-1,3,4-thiadiazoline-2-sulfonamide afforded two series of benzolamide analogues to which the carboxyl moiety has been derived as esters or amides, in order to reduce their very polar character. The new derivatives showed low nanomolar affinity for three carbonic anhydrase (CA) isozymes, CA I, II and IV, and were effective as topical antiglaucoma agents in normotensive rabbits. Efficacy of several of the new sulfonamides reported was better than that of the standard drugs dorzolamide and brinzolamide, whereas their duration of action was prolonged as compared to that of the clinically used drugs.
Dr. C.T. Supuran, Universita degli Studi, Lab. di Chim. Inorg. e Bioinorganica, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
Classification:
11.5.2 Topical (Part of: 11 Medical treatment > 11.5 Carbonic anhydrase inhibitors)
