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Abstract #8991 Published in IGR 5-2
Effects of 5-perfluorophenyl/octyl/butyl substituted derivatives of aromatic/heterocyclic sulfonamides on carbonic anhydrase II activity in vitro and on betamethasone induced ocular hypertension in rabbits
Di Filippo C; Rossi S; Lampa E; Boldrini E; Rinaldi B; Falcone G; Mazzeo F; Filippelli W; D'Amico MResearch Communications in Pharmacology and Toxicology 2002; 7: 101-110
5-perfluorophenyl/octyl/butyl substituted (compouds 1, 2 and 3, respectively) derivatives of aromatic/heterocyclic sulfonamides are newly synthesized compounds with putative reductive effect on the carbonic anhydrase activity and putative ocular hypotensive properties. Here, the authors studied the effects of these compounds on carbonic anhydrase II activity in vitro and on betamethasone induced ocular hypertension in rabbits. Compound 3 was found to be effective inhibitor of the CAII in vitro. In contrast, compound 1 showed significant activity at the highest (25 μm) dose tested, while no significant effect was observed for compound 2, In vivo, the administration of compounds 1 and 3, 1% and 2% (0.05 ml/day/twice a day) concentrations, significantly reduced the ocular hypertension induced by 20 days treatment with betamethasone into the eye. This effect started one hour after treatment on day 1, and lasted for 12 hours. In particular, the 1% concentration lowering activity was almost extinguished 12 hours later. A similar trend for IOP reduction was observed on days 10 and 20 of treatment. In contrast, the administration of compound 2 (2% solution) only occasionally reduced the ocular hypertension induced by betamethasone in rabbits. Therefore, the authors suggest the possible effectiveness of compound 3 (5-perfluorobutyl derivatized), and partially compound 1 (5-perfluorophenyl derivatized), as carbonic anhydrase inhibitors. They are active as topical intraocular pressure lowering agents in betamethasone-induced ocular hypertension.
Dr. C. Di Filippo, Department of Experimental Medicine, Faculty of Medicine and Surgery, 2nd University of Naples, Via Costantinopoli 16, 80138 Naples, Italy
Classification:
11.5.2 Topical (Part of: 11 Medical treatment > 11.5 Carbonic anhydrase inhibitors)
