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

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

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

J Med Chem. 1987 Apr;30(4):591-7.

PubMed ID
3560154 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EthoxzolamideCarbonic anhydrase 2Ki (nM)49000000N/AN/ADetails