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© Research
Publication : Journal of medicinal chemistry

Structure-activity relationship in PAF-acether. 3. Hydrophobic contribution to agonistic activity

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Scientific Fields
Diseases
Organisms
Applications
Technique

Published in Journal of medicinal chemistry - 01 May 1987

Godfroid JJ, Broquet C, Jouquey S, Lebbar M, Heymans F, Redeuilh C, Steiner E, Michel E, Coeffier E, Fichelle J

Link to Pubmed [PMID] – 3572968

J. Med. Chem. 1987 May;30(5):792-7

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.