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N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists
- Source :
- Bioorganicmedicinal chemistry letters. 16(22)
- Publication Year :
- 2006
-
Abstract
- A new class of potent NK3R antagonists based on the N',2-diphenylquinoline-4-carbohydrazide core is described. In an ex vivo assay in gerbil, the lead compound 2g occupies receptors within the CNS following oral dosing (Occ(90) 30 mg/kg po; plasma Occ(90) 0.95 microM) and has good selectivity and promising PK properties.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Administration, Oral
CHO Cells
Carbohydrazide
Gerbil
Biochemistry
Chemical synthesis
chemistry.chemical_compound
Structure-Activity Relationship
Cricetinae
Drug Discovery
Tumor Cells, Cultured
Structure–activity relationship
Animals
Receptor
Molecular Biology
Neurotransmitter Agents
Dose-Response Relationship, Drug
Organic Chemistry
Antagonist
Receptors, Neurokinin-3
Hydrazines
chemistry
Quinolines
Molecular Medicine
Lead compound
Ex vivo
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Issue :
- 22
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....b1d67d6296182f7a7db3242e6f7a3dd6