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Bioorg Med Chem Lett. 2012 Jan 15;22(2):1061-7. doi: 10.1016/j.bmcl.2011.11.112. Epub 2011 Dec 8.

Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency.

Author information

1
Department of Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States. wqian@amgen.com

Abstract

In a series of bradykinin B1 antagonists, we discovered that replacement of oxopiperazine acetamides with dehydro-oxopiperazine acetamides provided compounds with enhanced activity against the B1 receptor. The synthesis and SAR leading to potent analogs with reduced molecular weight will be discussed.

PMID:
22197141
DOI:
10.1016/j.bmcl.2011.11.112
[Indexed for MEDLINE]

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