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• W2051910820 abstract "In an effort to design new hybrid compounds with dual properties, i.e. binding affinity at histamine H3 receptors and inhibitory potency at the catabolic enzyme histamine Nτ-methyltransferase (HMT), a novel series of 1-substituted piperidine derivatives was synthesized. This alicyclic heterocycle is structurally linked via aminoalkyl spacers of variable lengths to additional aromatic carbo- or hetero-cycles. These new hybrid drugs were pharmacologically evaluated regarding their binding affinities at recombinant human H3 receptors, stably expressed in CHO cells, and in a functional assay for their inhibitory potencies at rat kidney HMT. All compounds investigated proved to be H3 receptor ligands with binding affinities in the micro- to nanomolar concentration range despite significant differences in the type of the aromatic moiety introduced. The most potent compound in this series was the quinoline derivative 20 (Ki = 5.6 nM). Likewise, all new ligands studied showed impressive HMT inhibitory activities. Here, compounds 5, 10, 14 and 18—20 exhibited submicromolar potencies (IC50 = 0.061—0.56 μM). The aminomethylated quinoline 19 showed almost the same, well balanced nanomolar activities on both targets. In this study, new hybrid compounds with a dual mode biological action were developed. These pharmacological agents are valuable leads for further development and candidates for treatment of histamine-dependent disorders." @default.
• W2051910820 created "2016-06-24" @default.
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• W2051910820 date "2004-10-01" @default.
• W2051910820 modified "2023-09-27" @default.
• W2051910820 title "Search for Histamine H₃Receptor Ligands with Combined Inhibitory Potency at Histamine<i>N</i>-Methyltransferase: ω-Piperidinoalkanamine Derivatives" @default.
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• W2051910820 doi "https://doi.org/10.1002/ardp.200400897" @default.
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