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Azaindoles as potent CRTH2 receptor antagonists
- Source :
- Bioorganicmedicinal chemistry letters. 21(2)
- Publication Year :
- 2010
-
Abstract
- A new class of 7-azaindole analogs of MK-7246 as potent and selective CRTH2 antagonists is reported. The SAR leading to the identification of the optimal azaindole regioisomer as well as the pharmacokinetics and off-target activities of the most potent antagonists are disclosed.
- Subjects :
- Indoles
Stereochemistry
medicine.drug_class
Clinical Biochemistry
Receptors, Prostaglandin
Pharmaceutical Science
Carboxamide
Biochemistry
Chemical synthesis
Rats, Sprague-Dawley
chemistry.chemical_compound
Structure-Activity Relationship
Pharmacokinetics
In vivo
Drug Discovery
medicine
Animals
Humans
Receptors, Immunologic
Receptor
Molecular Biology
Chemistry
Organic Chemistry
Antagonist
In vitro
Rats
Molecular Medicine
Prostaglandin D2
Carbolines
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 21
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....71d04c4cb50fd4d1ddbb29092b2c4143