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Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Jan 01; Vol. 26 (1), pp. 105-9. Date of Electronic Publication: 2015 Nov 10. - Publication Year :
- 2016
-
Abstract
- A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was identified. Selectivity and pharmacokinetic profiles of this compound are discussed.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Benzoates chemical synthesis
Benzoates chemistry
Dose-Response Relationship, Drug
Humans
Molecular Structure
Naphthalenes chemical synthesis
Naphthalenes chemistry
Structure-Activity Relationship
Benzoates pharmacology
Drug Discovery
Naphthalenes pharmacology
Receptors, Prostaglandin E, EP4 Subtype antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 26
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26608552
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.11.023