3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation

…, T Nguyen, DC D'Amico, W Qian, J Human…

文献索引：Chen, Jian Jeffrey; Nguyen, Thomas; D'Amico, Derin C.; Qian, Wenyuan; Human, Jason; Aya, Toshihiro; Biswas, Kaustav; Fotsch, Christopher; Han, Nianhe; Liu, Qingyian; Nishimura, Nobuko; Peterkin, Tanya A.N.; Yang, Kevin; Zhu, Jiawang; Riahi, Babak Bobby; Hungate, Randall W.; Andersen, Neil G.; Colyer, John T.; Faul, Margaret M.; Kamassah, Augustus; Wang, Judy; Jona, Janan; Kumar, Gondi; Johnson, Eileen; Askew, Benny C. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 11 p. 3384 - 3389

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被引用次数: 7

摘要

Abstract The discovery of novel and highly potent oxopiperazine based B1 receptor antagonists is described. Compared to the previously described arylsulfonylated (R)-3- amino-3-phenylpropionic acid series, the current compounds showed improved in vitro potency and metabolic stability. Compound 17, 2-((2R)-1-((4-methylphenyl) sulfonyl)-3-oxo- 2-piperazinyl)-N-((1R)-6-(1-piperidinylmethyl)-1, 2, 3, 4-tetrahydro-1-naphthalenyl) ...