Document Report Card

ID: ALA1124376

Journal: J Med Chem

Title: Topically active carbonic anhydrase inhibitors. 2. Benzo[b]thiophenesulfonamide derivatives with ocular hypotensive activity.

Authors: Graham SL, Shepard KL, Anderson PS, Baldwin JJ, Best DB, Christy ME, Freedman MB, Gautheron P, Habecker CN, Hoffman JM.

Abstract: Derivatives of benzo[b]thiophene-2-sulfonamide were prepared to investigate their potential utility as topically active inhibitors of ocular carbonic anhydrase. Such an agent would be useful in the treatment of glaucoma. Among the compounds described are 6-hydroxybenzo[b]thiophene-2-sulfonamide (16) and its acetate ester (23), which are among the most potent ocular hypotensive agents in this class, as assessed in the alpha-chymotrypsinized rabbit. These compounds were selected for clinical evaluation.

CiteXplore: 2585443

DOI: 10.1021/jm00132a009