Document Report Card

ID: ALA1125318

Journal: J Med Chem

Title: 4-substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors.

Authors: Hartman GD, Halczenko W, Smith RL, Sugŕue MF, Mallorga PJ, Michelson SR, Randall WC, Schwam H, Sondey JM.

Abstract: A series of 4-substituted thiophene- and furan-2-sulfonamides was prepared and was found to possess nanomolar-level potency for inhibition of human carbonic anhydrase II in vitro. Selected examples from this group were further evaluated for their potential to act as topically effective ocular hypotensive agents in the ocular normotensive albino rabbit and the ocular alpha-chymotrypsinized rabbit. Solubility studies in water and pH 7.4 buffer were carried out to estimate the ability of compounds to be formulated in solution. The sensitization potential of key representative structures was determined by in vitro glutathione reactivity studies and guinea pig maximization testing.

CiteXplore: 1433194

DOI: 10.1021/jm00099a010