Journal of Medicinal Chemistry p. 1196 - 1200 (1983)
Update date:2022-08-02
Topics: Inhibitors Derivatives 4-substituted
Williams, H. W. R.
Eichler, E.
Randall, W. C.
Rooney, C. S.
Cragoe, E. J.
et al.
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 * 10-8 M.
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