| Literature DB >> 22189275 |
Junya Shirai1, Hideyuki Sugiyama, Shinji Morimoto, Hironobu Maezaki, Yasuharu Yamamoto, Satoshi Okanishi, Izumi Kamo, Shiho Matsumoto, Keiko Ishigami, Nobuhiro Inatomi, Akio Imanishi, Makiko Kawamoto, Naoki Tarui, Tadatoshi Hashimoto, Yoshinori Ikeura.
Abstract
The synthesis and biological evaluation of a series of novel 3-phenylpiperidine-4-carboxamide derivatives are described. These compounds are generated by hybridization of the substructures from two types of tachykinin NK(1) receptor antagonists. Compound 42 showed high metabolic stability and excellent efficacy in the guinea-pig GR-73637-induced locomotive activity assay at 1 and 24h after oral administration. It also exhibited good pharmacokinetic profiles in four animal species, and a low potential in a pregnane X receptor induction assay.Entities:
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Year: 2011 PMID： 22189275 DOI： 10.1016/j.bmc.2011.11.048
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641