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Journal of medicinal chemistry

Inhibition of liver alcohol dehydrogenase and ethanol metabolism by 3-substituted thiolane 1-oxides

VK Chadha, KG Leidal, BV Plapp

文献索引:Chadha, Vijay K.; Leidal, Kevin G.; Plapp, Bryce V. Journal of Medicinal Chemistry, 1985 , vol. 28, # 1 p. 36 - 40

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被引用次数: 13

摘要

3-Substituted thiolane 1-oxides (methyl, n-butyl, n-hexyl, and phenyl) were prepared and tested as inhibitors of horse, monkey, and rat liver alcohol dehydrogenases and of ethanol metabolism in rats. These compounds inhibit alcohol oxidation in an uncompetitive manner with respect to ethanol as a varied suibstrate. Lengthening the alkyl substituent increased the inhibitory potency because of tighter binding in the hydrophobic substrate binding ...