Structure-activity relationship in PAF-acether. 3. Hydrophobic contribution to agonistic activity.
The synthesis of some selected PAF-acether homologues with an alkoxy-chain length from C1 to C20 in position 1 is described. All agonist activities are closely correlated among themselves and with the calculated fatty-chain hydrophobicity. After a discussion on recent published results and comparison with our data, we conclude that the ether oxide function is absolutely essential at the glycerol 1-position for potent agonist activity and that potency correlates well with hydrophobicity parameters. We indicate the importance of steric and configurational constraints.
D000818:Animals; D001794:Blood Pressure; D001980:Bronchi / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D003251:Constriction, Pathologic / Q000139:chemically induced; D006168:Guinea Pigs; D008297:Male; D008968:Molecular Conformation; D010972:Platelet Activating Factor / Q000502:physiology*; D010974:Platelet Aggregation; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D013921:Thrombocytopenia / Q000139:chemically induced
D010972:Platelet Activating Factor