Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists

Our first generation CRTH2 and DP dual antagonists, represented by AMG 009, are more potent toward the CRTH2 receptor than to the DP receptor. Here we report our efforts in the discovery of CRTH2 and DP dual antagonists with more balanced potencies to both receptors, such as compound 15. Our first g...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-02, Vol.22 (4), p.1686-1689
Hauptverfasser:	Liu, Jiwen (Jim), Wang, Yingcai, Johnson, Michael G., Li, An-Rong, Shen, Wang, Wang, Xuemei, Su, Yongli, Brown, Matthew, Van Lengerich, Bettina, Rickel, Erika, Martin, Tod, Budelsky, Alison, Seitz, Lisa, Danao, Jay, Tang, H. Lucy, Collins, Tassie, Medina, Julio C.
Format:	Artikel
Sprache:	eng
Schlagworte:	antagonists Asthma Biological and medical sciences chemistry CRTH2 Drug Design Dual Antagonist GPCR HEK293 Cells Humans Inhibitory Concentration 50 Medical sciences Molecular Structure PGD2 Pharmacology. Drug treatments Phenylacetates - chemical synthesis Phenylacetates - chemistry Phenylacetates - pharmacology phenylacetic acid Protein Binding - drug effects receptors Receptors, Immunologic - antagonists & inhibitors Receptors, Prostaglandin - antagonists & inhibitors SAR
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Zusammenfassung:	Our first generation CRTH2 and DP dual antagonists, represented by AMG 009, are more potent toward the CRTH2 receptor than to the DP receptor. Here we report our efforts in the discovery of CRTH2 and DP dual antagonists with more balanced potencies to both receptors, such as compound 15. Our first generation CRTH2 and DP dual antagonists, represented by AMG 009, are more potent toward the CRTH2 receptor than to the DP receptor. Here we report our efforts in the discovery of CRTH2 and DP dual antagonists with more balanced potencies to both receptors, such as compound 15.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.12.107