Compounds for inhibition of platelet activating factor activity

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – C-o-group doai

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514834, 514929, 514930, 514870, A01N 3100

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active

048514500

ABSTRACT:
The present invention is a group of biologically active agents, di-hydroxy alkyl glycerols with vicinal hydroxyl groups and their acetyl-derivatives having the general formula: ##STR1## where R is selected from the group of H and CH.sub.3 CO-- and x+y is between 9 and 21; and methods for their synthesis. The compounds of the present invention are synthesized starting with an unsaturated 1-O-alkyl-glycerol of the formula: ##STR2## where R is an unsaturated alkyl group with a chain length of 12 to 24 carbon atoms and introducing a vicinal hydroxyl into the alkyl carbon chain using either osmium tetroxide or performic acid, produced by mixing formic acid with hydrogen peroxide.
The new glycerol ether derivatives exert platelet activating factor (PAF)-like action in vitro in low concentrations, and, surprisingly, in higher doses act as selective antagonists of PAF, or 1-O-alkyl-2-O-acetyl-sn-glyceryl-3-phosphorylcholine (AGEPC), activities. These compounds are therefore useful under some conditions in the prevention and/or treatment of the undesirable effects of PAF secretion, including platelet aggregation, serotonin secretion, and decreased systolic blood pressure.

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Tselepis, et al., Comp. Biochem. Physiol. 87C(1), 41-46 (1987).
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Bergmeyer et al., "Methods of Enzymatic Analysis", 3, 1196, Academic Press, N.Y. (1974).
Tang et al., Chemistry and Physics of Lipids 17, 169-175 (1976).

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