Document Report Card

ID: ALA1124833

Journal: J Med Chem

Title: Topically active carbonic anhydrase inhibitors. 3. Benzofuran- and indole-2-sulfonamides.

Authors: Graham SL, Hoffman JM, Gautheron P, Michelson SR, Scholz TH, Schwam H, Shepard KL, Smith AM, Smith RL, Sondey JM.

Abstract: 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.

CiteXplore: 2299640

DOI: 10.1021/jm00164a045