
European Journal of Medicinal Chemistry p. 609 - 615 (1990)
Update date:2022-08-02
Topics:
Ilagouma, A. T.
Dornand, J.
Liu, C. F.
Zenone, F.
Mani, J. C.
Kamenka, J. M.
Derivatives and analogues of the phencyclidine molecule (1-phenyl 1-(1-piperidino) cyclohexane or PCP) were prepared to investigate their immunosuppressive potency and to define the physicochemical parameters which may influence this activity recently demonstrated for PCP.Most of the tested molecules are more effective than PCP itself.In spite of lack of quantitative data, the biological activity appears to be dependent upon 3 parameters: conformation, lipophilicity, and the empirical Hammett's parameters.The homogeneous conformations with a high lipophilicity were the most immunosuppressive.Interestingly, such structures appeared to be of weak potency on the PCP receptor in the CNS.
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