Casini, Angela ![]() |
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: | 31 Oct 2022 10:38 |
URI: | https://orca.cardiff.ac.uk/id/eprint/85544 |
Citation Data
Cited 36 times in Scopus. View in Scopus. Powered By Scopus® Data
Actions (repository staff only)
![]() |
Edit Item |