| Literature DB >> 21514825 |
Jian Jeffrey Chen1, Thomas Nguyen, Derin C D'Amico, Wenyuan Qian, Jason Human, Toshihiro Aya, Kaustav Biswas, Christopher Fotsch, Nianhe Han, Qingyian Liu, Nobuko Nishimura, Tanya A N Peterkin, Kevin Yang, Jiawang Zhu, Babak Bobby Riahi, Randall W Hungate, Neil G Andersen, John T Colyer, Margaret M Faul, Augustus Kamassah, Judy Wang, Janan Jona, Gondi Kumar, Eileen Johnson, Benny C Askew.
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)acetamide, showed EC(50) of 10.3 nM in a rabbit biochemical challenge model. The practical syntheses of chiral arylsulfonylated oxopiperazine acetic acids are also described.Entities:
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Year: 2011 PMID： 21514825 DOI： 10.1016/j.bmcl.2011.03.115
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823