Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors.
Article Details
- CitationCopy to clipboard
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
Drug Target Property Measurement pH Temperature (°C) Ethoxzolamide Carbonic anhydrase 2 Ki (nM) 49000000 N/A N/A Details