Cleavage of carbon-carbon bonds with high stereochemical control. 7. Chiral .alpha.-silyl benzoylcycloalkanes undergo base-catalyzed cleavage with retention of configuration when not sterically congested
Cleavage of carbon-carbon bonds with high stereochemical control. 7. Chiral .alpha.-silyl benzoylcycloalkanes undergo base-catalyzed cleavage with retention of configuration when not sterically congested
A HINDERED PHENOL COMPOUND, PREPARATION THEREOF AND USE THEREOF AS AN ANTIOXIDANT
申请人:China Petroleum & Chemical Corporation
公开号:EP2952505B1
公开(公告)日:2018-05-23
A Convenient Method for the Synthesis of Diiodo Compounds. Facile Cleavage of Cyclic Ethers by Phenyl Dichlorophosphate and Sodium Indide
作者:Hsing-Jang Liu、Lisa M. Shewchuk、Montse Llinas-Brunet
DOI:10.3987/r-1986-11-3043
日期:——
Inhibition of liver alcohol dehydrogenase and ethanol metabolism by 3-substituted thiolane 1-oxides
作者:Vijay K. Chadha、Kevin G. Leidal、Bryce V. Plapp
DOI:10.1021/jm00379a009
日期:1985.1
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 substrate. Lengthening the alkyl substituent increased the inhibitory potency because of tighter binding in the hydrophobic substrate binding pocket of the alcohol dehydrogenases. Thus, the 3-hexyl derivative was the most potent inhibitor of the purified rat liver alcohol dehydrogenase, with a Kii value of 0.13 microM. The 3-butyl derivative was the best inhibitor of ethanol metabolism in rats, with a Kii value of 11 mumol/kg. The acute toxicity in mice of the butyl derivative was 1.4 mmol/kg. Since high concentrations of alcohol do not prevent the inhibitory effects of these compounds, they may be particularly useful for preventing poisoning by methanol or ethylene glycol.
Synthesis and biological evaluation of 9-(5′,5′-difluoro-5′-phosphonopentyl)guanine derivatives for PNP-inhibitors
9-(5',5'-Difluoro-5'-phosphonopentyl)guanine (DFPP-G) and its hypoxanthine analogue (DFPP-H) were modified by introducing a methyl group to all possible positions of the linker connecting a purine and difluoromethylenephosphonic acid moiety to evaluate the effects of the methyl group on inhibition against purine nucleoside phosphorylase. The methyl group on the linker affected the inhibition in a positional-dependent manner. Inhibitory potency of alpha-methyl and beta-methyl -substituted analogues of DFPP-H increased by about 600- to 1000-fold upon converting to cyclopropane nucleotide analogue (+/-)-4. (c) 2005 Elsevier Ltd. All rights reserved.