Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism

Bioorg Med Chem Lett. 2012 Jan 1;22(1):367-70. doi: 10.1016/j.bmcl.2011.10.123.

Yingcai Wang ¹, Zice Fu, Michael Schmitt, Xuemei Wang, Wang Shen, Erika Rickel, Tod Martin, Alison Budelsky, Derek Marshall, Tassie Collins, H Lucy Tang, Julio C Medina, Jiwen Jim Liu

Affiliations

Affiliation

1 Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA.

PMID: 22119474 DOI: 10.1016/j.bmcl.2011.10.123

Abstract

We have previously reported that optimization of a series of phenylacetic acid derivatives led to the discovery of CRTH2 and DP dual antagonists, such as AMG 009 and AMG 853. During the optimization process, we discovered that minor structural modifications also afforded potent and selective CRTH2 or DP antagonists. Here we report the structure-activity relationship that led to the discovery of selective CRTH2 antagonists such as 2 and 17, and selective DP antagonists, such as 4 and 5.

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