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New indole amide derivatives as potent CRTH2 receptor antagonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 21:3471-3474
- Publication Year :
- 2011
- Publisher :
- Elsevier BV, 2011.
-
Abstract
- A new series of indole amide acting as hCRTH2 receptor ligands had been explored and are described herein. Several amide derivatives displaying low nanomolar activity in hCRTH2 binding and whole blood assays were identified. They were found to behave as a full antagonists, exhibiting good selectivity over related prostaglandin receptors. Also, prototypical compounds in this novel series which displayed acceptable CYP profiles and were orally bioavailable in rats were identified.
- Subjects :
- Indoles
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Prostaglandin
Ligands
Biochemistry
Chemical synthesis
Inhibitory Concentration 50
chemistry.chemical_compound
Amide
Drug Discovery
Animals
Receptor
Molecular Biology
Indole test
Molecular Structure
biology
Receptors, Dopamine D2
Chemistry
Organic Chemistry
Cytochrome P450
Amides
Rats
biology.protein
Molecular Medicine
Prostaglandin D2
Selectivity
Protein Binding
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....a09028c83914f05337f367fe720b7f52
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.03.085