Godfroid J J, Broquet C, Jouquey S, Lebbar M, Heymans F, Redeuilh C, Steiner E, Michel E, Coeffier E, Fichelle J
J Med Chem. 1987 May;30(5):792-7. doi: 10.1021/jm00388a008.
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.
