(+)-(2R, 5S)-4-[4-Cyano-3-(trifluoromethyl) phenyl]-2, 5-dimethyl-N-[6-(trifluoromethyl) pyridin-3-yl] piperazine-1-carboxamide (YM580) as an Orally Potent and …

…, A Matsuhisa, K Samizu, E Kawanimani…

文献索引：Kinoyama, Isao; Taniguchi, Nobuaki; Toyoshima, Akira; Nozawa, Eisuke; Kamikubo, Takashi; Imamura, Masakazu; Matsuhisa, Akira; Samizu, Kiyohiro; Kawanimani, Eiji; Niimi, Tatsuya; Hamada, Noritaka; Koutoku, Hiroshi; Furutani, Takashi; Kudoh, Masafumi; Okada, Minoru; Ohta, Mitsuaki; Tsukamoto, Shin-Ichi Journal of Medicinal Chemistry, 2006 , vol. 49, # 2 p. 716 - 726

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被引用次数: 26

摘要

A novel series of trans-N-aryl-2, 5-dimethylpiperazine-1-carboxamide derivatives was synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic effects were evaluated. Pharmacological assays indicated that compound 33 was a potent AR antagonist, and subsequent optical resolution provided (+)-(2R, 5S)-4-[4- cyano-3-(trifluoromethyl) phenyl]-2, 5-dimethyl-N-[6-(trifluoromethyl) pyridin-3-yl] ...