[PAF-antagonists with lipid structure. 6. Alkylpropandiol lipids with acyl- and ether- structures at the C-3 position and heterocyclic head groups; synthesis, characterization and structure-activity relationship].
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).
Kertscher
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Pharmazeutisches Institut, Universität Leipzig, Germany.
D001792:Blood Platelets / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D010972:Platelet Activating Factor / Q000037:antagonists & inhibitors*; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D011409:Propylene Glycols / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors; D011409:Propylene Glycols