Author/Authors :
Sunil Paliwal، نويسنده , , Gregory A. Reichard، نويسنده , , Sapna Shah، نويسنده , , Michelle Laci Wrobleski، نويسنده , , Cheng Wang، نويسنده , , Carmine Stengone، نويسنده , , Hon-Chung Tsui، نويسنده , , Dong Xiao، نويسنده , , Ruth A. Duffy، نويسنده , , Jean E. Lachowicz، نويسنده , , Amin A. Nomeir، نويسنده , , Geoffrey B. Varty، نويسنده , , Neng-Yang Shih، نويسنده ,
Abstract :
Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and orally more efficacious γ-lactam series of selective NK1 antagonists. Optimization of the lactam series culminated in the identification of compounds with high binding affinity and excellent oral CNS activity.
Keywords :
Emesis , Substance P , CNS , NK1 , lactam
