Department of Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States.
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1061-7. doi: 10.1016/j.bmcl.2011.11.112. Epub 2011 Dec 8.
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.
在一系列缓激肽 B1 拮抗剂中，我们发现用去氢-氧哌嗪乙酰胺取代氧哌嗪乙酰胺可提供对 B1 受体活性增强的化合物。将讨论导致具有降低分子量的有效类似物的合成和 SAR。
