78945-91-2

Upstream product

• 78945-97-8 2-metil-3-carbossimetil-4-fenil-1,2-diidro-1-ossiisochinolina 
• 78945-99-0 1-oxo-4-phenyl-1,2-dihydroisoquinoline-3-carboxylic acid 
• 69454-47-3 3-carbossimetil-4-fenil-1,2-diidro-1-ossiisochinolina 
• 37617-98-4 4-phenyl-3-isocoumarincarboxylic acid 
• 78945-92-3 1,2-dihydro-2-methyl-1-oxo-4-phenyl-3-isoquinolinecarboxylic acid 

Downstream Products

• 125064-54-2 3-(hydroxymethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone 
• 159819-94-0 3-<<(methylsulfonyl)oxy>methyl>-2-methyl-4-phenyl-1(2H)-isoquinolinone 
• 1027396-00-4 (2-Methyl-1-oxo-4-phenyl-1,2-dihydro-isoquinolin-3-yl)-acetyl chloride 
• 167756-82-3 1,2-dihydro-2-methyl-1-oxo-4-phenyl-3-isoquinolineacetic acid 
• 167756-81-2 1,2-dihydro-2-methyl-1-oxo-4-phenyl-1(2H)-isoquinolineacetonitrile 
• 1027146-46-8 1,2-dihydro-N,2-dimethyl-1-oxo-4-phenyl-3-isoquinolinemethylamine 
• 164934-89-8 2-methyl-1-oxo-1,2-dihydro-3-carbazoyl-4-phenylisoquinoline 

Relevant academic research and scientific papers

Novel, Potent, and Orally Active Substance P Antagonists: Synthesis and Antagonist Activity of N-Benzylcarboxamide Derivatives of Pyridopyridine

A series of 4-phenylisoquinolone derivatives were synthesized and evaluated for NK1 (substance P) antagonist activity.Highly potent antagonists, 4-phenyl-3-isoquinolone-N-benzylcarboxamides (11), were discovered from the structure-activity relationship studies on the isoquinolone-urea lead 1a.Optimization of the activity in this series resulted in the development of 5-phenyl-6-pyridopyridine-N-benzylcarboxamides (30) which are highly potent orally active NK1 antagonists.Among the compounds synthesized, N--7,8-dihydro-N,7-dimethyl-8-oxo-5-(substituted phenyl)-6-pyridopyridinecarboxamides (30a,f,g) showed excellent antagonist activities with IC50 values (in vitro inhibition of 125I>BH-SP binding in human IM-9-cells) of 0.21-0.34 nM and ED50 values (in vivo inhibition of capsaicin-induced plasma extravasation in guinea-pig trachea, iv) of 0.017-0.030 mg/kg.These compounds exhibited significantly potent activity upon oral adiministration with ED50 values of 0.068-0.17 mg/kg.Conformational studies on 30g indicated that the two stable conformers of 30g are quite similar to those of CP-99,994.