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

JJ Godfroid, C Broquet, S Jouquey…

文献索引:Godfroid, Jean-Jacques; Broquet, Colette; Jouquey, Simone; Lebbar, Mariya; Heymans, Francoise; et al. Journal of Medicinal Chemistry, 1987 ,  vol. 30,  # 5  p. 792 - 797

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被引用次数: 26

摘要

The synthesis of some selected PAF-acether homologues with an alkoxy-chain length from C1 to C,, 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 ...