European Journal of Medicinal Chemistry p. 1710 - 1717 (2009)
Update date:2022-07-30
Topics:
Herold, Franciszek
Chodkowski, Andrzej
Izbicki, Lukasz
Krol, Marek
Kleps, Jerzy
Turlo, Jadwiga
Nowak, Gabriel
Stachowicz, Katarzyna
Dybala, Malgorzata
Siwek, Agata
A series of new derivatives of 4-aryl-pyrido[1,2-c]pyrimidine containing the 3-(4-piperidyl)-1H-indole residue or its 5-methoxy derivative were synthesized. They were characterized (i) in vitro by binding to 5-HT1A receptors and 5-HT transporter proteins in rat brain cortex membranes and (ii) in vivo in the mouse by induced hypothermia and forced swimming models for antagonist/agonist activity against the 5-HT1A autoreceptors and postsynaptic 5-HT1A receptors, respectively. Structure activity relationship evaluation indicated that the presence of the 3-(4-piperidyl)-1H-indole residue and ortho- or para-substituents with -F or -CH3 groups in the aryl ring as well as an unsubstituted aryl in the 4-aryl-pyrido[1,2-c]pyrimidine moiety promoted low Ki values for both receptors. In contrast, the presence of a 5-methoxy-3-(4-piperidyl)-1H-indole residue as well as -Cl or -OCH3 substituents at the para position markedly reduced the receptor affinity.
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