Document Report Card

ID: ALA1123900

Journal: J Med Chem

Title: Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors.

Authors: Ponticello GS, Freedman MB, Habecker CN, Lyle PA, Schwam H, Varga SL, Christy ME, Randall WC, Baldwin JJ.

Abstract: An attempt to develop a water-soluble carbonic anhydrase inhibitor focused on exploring structure-activity relationships in the thienothiopyransulfonamide class. The strategy to influence water solubility while retaining carbonic anhydrase activity involved the introduction of a hydroxyl moiety and adjusting the oxidation state of the sulfur on the thiopyran portion of the molecule. Compounds 4 and 17 best fit the criteria of aqueous solubility and inhibitory potency vs. human carbonic anhydrase II and are candidates for evaluation as topically effective antiglaucoma agents.

CiteXplore: 3560154

DOI: 10.1021/jm00387a002