发现去氢氧哌嗪乙酰胺类新型缓激肽 B1 受体拮抗剂，体外活性增强。
Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency.
机构信息
Department of Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, United States.
出版信息
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1061-7. doi: 10.1016/j.bmcl.2011.11.112. Epub 2011 Dec 8.
PMID:22197141
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.
摘要
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。
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