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 receptor (hHR) were evaluated. Among them, 4-(cyclohexylmethyl)-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine (14) exhibited hHR affinity with a K of 160 nM and behaved as antagonist in functional assays: the cellular aequorin-based assay (IC = 32 nM) and [S]GTPγS binding assay (pK = 6.67). In addition, antinociceptive activity of 14in vivo was observed in Formalin test (in mice) and in Carrageenan-induced acute inflammation test (in rats).
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| http://dx.doi.org/10.1016/j.bmc.2019.02.020 | DOI Listing |
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