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Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands.

Abstract：

:A series of novel 2-amino-4-(4-methylpiperazin-1-yl)-1,3,5-triazine derivatives with different aryl substituents in the 6-position was designed, synthesized and evaluated for histamine H4 receptor (H4R) affinity in Sf9 cells expressing human H4R co-expressed with G-protein subunits. Triazine derivative 8 with a 6-(p-chlorophenyl) substituent showed the highest affinity with hH4R Ki value of 203 nM and was classified as an antagonist in cAMP accumulation assay. This compound, identified as a new lead structure, demonstrated also anti-inflammatory properties in preliminary studies in mice (carrageenan-induced edema test) and neither possessed significant antiproliferative activity, nor modulated CYP3A4 activity up to concentration of 25 μM. In order to discuss structure-activity relationships molecular modeling and docking studies were undertaken.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Łażewska D,Więcek M,Ner J,Kamińska K,Kottke T,Schwed JS,Zygmunt M,Karcz T,Olejarz A,Kuder K,Latacz G,Grosicki M,Sapa J,Karolak-Wojciechowska J,Stark H,Kieć-Kononowicz K

doi

10.1016/j.ejmech.2014.06.032

subject

Has Abstract

pub_date

2014-08-18 00:00:00

pages

534-46

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(14)00551-0

journal_volume

83

pub_type

杂志文章

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