1149339-75-2Relevant articles and documents
Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT1A activity, Part 1
Herold, Franciszek,Chodkowski, Andrzej,Izbicki, Lukasz,Krol, Marek,Kleps, Jerzy,Turlo, Jadwiga,Nowak, Gabriel,Stachowicz, Katarzyna,Dybala, Malgorzata,Siwek, Agata
experimental part, p. 1710 - 1717 (2009/05/26)
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.
