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Topically active carbonic anhydrase inhibitors. 3. Benzofuran- and indole-2-sulfonamides. 1990
S L Graham, and
J M Hoffman, and
P Gautheron, and
S R Michelson, and
T H Scholz, and
H Schwam, and
K L Shepard, and
A M Smith, and
R L Smith, and
J M Sondey
Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, West Point, Pennsylvania 19486.
Derivatives of benzofuran- and indole-2-sulfonamide were prepared for evaluation as topically active ocular hypotensive agents. These compounds were found to be excellent inhibitors of carbonic anhydrase and to lower intraocular pressure in a rabbit model of ocular hypertension. However, the development of these compounds for clinical use was precluded by the observation that they cause dermal sensitization in guinea pigs. A correlation between electrophilicity, as assessed by in vitro reactivity with reduced glutathione, and dermal sensitization potential was further documented.
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