Design, structure–activity relationship, and highly efficient asymmetric synthesis of 3-phenyl-4-benzylaminopiperidine derivatives as novel neurokinin-1 receptor …

…, Y Yamamoto, M Kawamoto, N Tarui, I Kamo…

文献索引：Shirai, Junya; Yoshikawa, Takeshi; Yamashita, Masayuki; Yamamoto, Yasuharu; Kawamoto, Makiko; Tarui, Naoki; Kamo, Izumi; Hashimoto, Tadatoshi; Ikeura, Yoshinori Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 21 p. 6430 - 6446

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被引用次数: 3

摘要

We synthesized a series of novel 3-phenyl-4-benzylaminopiperidine derivatives that were identified as potent tachykinin NK1 receptor antagonists by structural modification of the 3- benzhydrylpiperidone derivative through high-throughput screening. N-{2-[(3R, 4S)-4-({2- Methoxy-5-[5-(trifluoromethyl)-1H-tetrazol-1-yl] benzyl} amino)-3-phenyl-1-piperidinyl]-2- oxoethyl} acetamide ((+)-39) was found to be one of the most potent tachykinin NK1 ...