Zusammenfassung
This study focuses on the design, synthesis, molecular modeling and biological evaluation of a novel group of alkyl-1,3,5-triazinyl-methylpiperazines. New compounds were synthesized and their affinities for human histamine H-4 receptor (hH(4)R) were evaluated. Among them, 4-(cyclohexylmethyl)-6-(4-methylpiperazin-1-yl)1,3,5- triazin-2-amine (14) exhibited hH(4)R affinity with a K-i of 160 nM and ...
Zusammenfassung
This study focuses on the design, synthesis, molecular modeling and biological evaluation of a novel group of alkyl-1,3,5-triazinyl-methylpiperazines. New compounds were synthesized and their affinities for human histamine H-4 receptor (hH(4)R) were evaluated. Among them, 4-(cyclohexylmethyl)-6-(4-methylpiperazin-1-yl)1,3,5- triazin-2-amine (14) exhibited hH(4)R affinity with a K-i of 160 nM and behaved as antagonist in functional assays: the cellular aequorin-based assay (IC50= 32 nM) and [S-35] GTP.S binding assay (pKb= 6.67). In addition, antinociceptive activity of 14 in vivo was observed in Formalin test (in mice) and in Carrageenan-induced acute inflammation test (in rats).
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