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Topical carbonic anhydrase inhibitors
Journal of Medicinal Chemistry1984Vol. 27(6), pp. 810–812
Citations Over TimeTop 11% of 1984 papers
Abstract
Ethoxzolamide and several derivatives (1-6) were synthesized and evaluated for carbonic anhydrase inhibition (CAI), solubility, pKa, distribution, and corneal permeability. The 6-hydroxy (5) and, particularly, the 6-chloro (6) analogues have the best combination of properties for penetrating the site of action and reducing intraocular pressure. Both 5 and 6 exhibited topical effectiveness in the normal rabbit, with 6 showing greater potency.
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