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

Authors :
Liu JJ
Wang Y
Johnson MG
Li AR
Shen W
Wang X
Su Y
Brown M
Van Lengerich B
Rickel E
Martin T
Budelsky A
Seitz L
Danao J
Tang HL
Collins T
Medina JC
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Feb 15; Vol. 22 (4), pp. 1686-9. Date of Electronic Publication: 2011 Dec 30.
Publication Year :
2012

Abstract

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.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
22
Issue :
4
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
22264478
Full Text :
https://doi.org/10.1016/j.bmcl.2011.12.107