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Optimization of phenylacetic acid derivatives for balanced CRTH2 and DP dual antagonists.
- 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.)
- Subjects :
- HEK293 Cells
Humans
Inhibitory Concentration 50
Molecular Structure
Phenylacetates chemistry
Phenylacetates pharmacology
Protein Binding drug effects
Drug Design
Phenylacetates chemical synthesis
Receptors, Immunologic antagonists & inhibitors
Receptors, Prostaglandin antagonists & inhibitors
Subjects
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