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).
Download full-text PDF |
Source |
---|
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!