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[PAF-antagonists with lipid structure. 6. Alkylpropandiol lipids with acyl- and ether- structures at the C-3 position
1Pharmazeutisches Institut, Universität Leipzig, Germany.
Die Pharmazie
|December 31, 1997
Abstract:
A series of 14 PAF-analogues with simple lipid structure and heterocyclic head groups were synthesized, and the PAF-inhibitory potencies on human blood platelets was evaluated in vitro. Structure-activity relationships revealed that the PAF-antagonist activity is strongly influenced by the distance between position C-3 of the backbone and onium center and the structure of the heterocyclus. The best activity showed the 3,5-dimethylpyridinium derivative with a distance of 5 methylene groups (IC50 = 0.8 mumol/l).