Analysis of crucial structural requirements of 2-substituted pyrimido[4,5-b][1,5]oxazocines as NK(1) receptor antagonist by axially chiral derivatives

Analysis of crucial structural requirements of 2-substituted pyrimido[4,5-b][1,5]oxazocines as NK(1) receptor antagonist by axially chiral derivatives

This study aimed to identify the crucial structural features of 2-substituted 8-methylpyrimido[4,5-b][1,5]oxazocine derivatives. Axially chiral 8-methylpyrimido[4,5-b][1,5]oxazocines bearing a substituent at the C-2 position were synthesized and evaluated as NK(1) antagonists. The results revealed t...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2007-08, Vol.15 (15), p.5083-5089
Hauptverfasser: Seto, Shigeki, Asano, Jun
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Dose-Response Relationship, Drug
Guinea Pigs
Ileum - drug effects
Molecular Structure
Muscle Contraction - drug effects
Muscle, Smooth - drug effects
Neurokinin-1 Receptor Antagonists
Oxazocines - chemistry
Oxazocines - pharmacology
Structure-Activity Relationship
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Zusammenfassung:This study aimed to identify the crucial structural features of 2-substituted 8-methylpyrimido[4,5-b][1,5]oxazocine derivatives. Axially chiral 8-methylpyrimido[4,5-b][1,5]oxazocines bearing a substituent at the C-2 position were synthesized and evaluated as NK(1) antagonists. The results revealed that (aR, 8S)-stereochemistry and the substituent at the C-2 position are important for NK(1) receptor recognition.
ISSN:0968-0896