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Carbonic anhydrase inhibitors: Topically acting antiglaucoma sulfonamides incorporating esters and amides of 3-and 4-carboxybenzolamide

Casini, Angela, Scozzafava, A, Mincione, F, Menabuoni, L, Starnotti, M and Supuran, C. T. 2003. Carbonic anhydrase inhibitors: Topically acting antiglaucoma sulfonamides incorporating esters and amides of 3-and 4-carboxybenzolamide. Biorganic and Medicinal Chemistry Letters 13 (17) , pp. 2867-2873. 10.1016/S0960-894X(03)00580-8

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Abstract

Reaction of 3- and 4-carboxybenzenesulfonyl chloride with 5-amino-1,3,4-thiadiazole-2-sulfonamide/5-imino-4-methyl-δ 2-1,3,4-thiadiazoline-2-sulfonamide afforded two series of benzolamide analogues to which the carboxyl moiety has been derivatized 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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
Subjects: Q Science > QD Chemistry
Uncontrolled Keywords: Administration, Topical; Animals; Benzolamide; Carbonic Anhydrase I; Carbonic Anhydrase II; Carbonic Anhydrase Inhibitors; Carbonic Anhydrase IV; Cattle; Esters; Glaucoma; Humans; Intraocular Pressure; Rabbits; Structure-Activity Relationship; Sulfonamides; Thiazines; Thiophenes
Publisher: Elsevier
ISSN: 0960-894X
Last Modified: 04 Jun 2017 08:49
URI: http://orca.cf.ac.uk/id/eprint/85544

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