Inhibitors of glycolic acid oxidase. 4-substituted 2,4-dioxobutanoic acid derivatives.
| Autor: | Williams HW, Eichler E, Randall WC, Rooney CS, Cragoe EJ Jr, Streeter KB, Schwam H, Michelson SR, Patchett AA, Taub D |
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| Jazyk: | angličtina |
| Zdroj: | Journal of medicinal chemistry [J Med Chem] 1983 Aug; Vol. 26 (8), pp. 1196-200. |
| DOI: | 10.1021/jm00362a020 |
| Abstrakt: | Fourteen new 4-substituted 2,4-dioxobutanoic acids have been synthesized. These compounds, all of which contain lipophilic 4-substituents, are potent inhibitors in vitro of porcine liver glycolic acid oxidase. The I50 value of the two most potent representatives, 4-(4'-bromo[1,1'-biphenyl]-4-yl)-2, 4-dioxobutanoic acid (8) and 4-[4'-[[(3,4-dihydro-3-hydroxy-2H-1, 5-benzodioxepin-3-yl)methyl]thio][1,1'-biphenyl]-4-yl]-2, 4-dioxobutanoic acid (13) is 6 X 10(-8)M. |
| Databáze: | MEDLINE |
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