Thienothiopyran-2-sulfonamides: novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma
| Autor: | W. C. Randall, Michael F. Sugrue, Gerald S. Ponticello, Harvey Schwam, Marcia E. Christy, P. S. Anderson, John J. Baldwin, James P. Springer, Murcko Mark A, P. Gautheron |
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| Rok vydání: | 1989 |
| Předmět: |
Bicarbonate
Molecular Conformation Iris Thiophenes Ciliary processes chemistry.chemical_compound Ciliary body In vivo Carbonic anhydrase Drug Discovery medicine Animals Humans Carbonic Anhydrase Inhibitors chemistry.chemical_classification Sulfonamides Binding Sites biology Chemistry Ciliary Body Glaucoma In vitro medicine.anatomical_structure Enzyme Biochemistry biology.protein Molecular Medicine Cattle Rabbits Ex vivo |
| Zdroj: | Journal of Medicinal Chemistry. 32:2510-2513 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00132a003 |
| Popis: | The bulk of aqueous humor entering the eye is produced through an active secretory process by the nonpigmented epithelial cells of the ciliary process. Carbonic anhydrase is present in these cells, and following inhibition of the enzyme, bicarbonate formation is decreased, which, in turn, diminishes sodium and fluid secretion into the eye. The biological profile of the thienothiopyrans was assessed through in vitro, ex vivo, and in vivo studies. In vitro determination of I 50 and K i values utilized HCA-II, the isozyme found in the human ciliary process |
| Databáze: | OpenAIRE |
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