当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. Part 5.

Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. Part 5.

Abstract：

:A series of novel 4-aryl-pyrido[1,2-c]pyrimidine derivatives containing a 1-(2-quinoline)piperazine moiety was synthesized. The chemical structure of new compounds was confirmed by FT-IR, (1)H NMR, (13)C NMR and HRMS spectra as well as elemental analysis. Affinity of the novel pyrido[1,2-c]pyrimidine derivatives for 5-HT1A, 5-HT2A receptors and serotonin transporter (SERT) was evaluated in an in vitro radioligand binding assay. Tested compounds showed moderate to high affinity for 5-HT1AR and SERT and low affinity for 5-HT2AR. Selected ligands were subjected to in vivo tests, such as induced hypothermia and the forced swimming test in mice, which determined presynaptic agonistic activity of the ligands 8d, 8e, 9d and 9e and presynaptic antagonistic activity of the ligands 8a, 8b, 9a, 9b. Additionally, metabolic stability evaluation was performed for selected ligands, proving that a para-substitution in the 4-aryl-pyrido[1,2-c]pyrimidine moiety leads to an increase in stability, whereas a substitution in the ortho-position lowers the stability.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Gomółka A,Ciesielska A,Wróbel MZ,Chodkowski A,Kleps J,Dawidowski M,Siwek A,Wolak M,Stachowicz K,Sławińska A,Nowak G,Satała G,Bojarski AJ,Belka M,Ulenberg S,Bączek T,Skowronek P,Turło J,Herold F

doi

10.1016/j.ejmech.2015.05.003

subject

Has Abstract

pub_date

2015-06-15 00:00:00

pages

221-36

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30030-1

journal_volume

98

pub_type

杂志文章

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