Title of article :
1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists
Author/Authors :
Sander G. Mills، نويسنده , , Malcolm MacCoss، نويسنده , , Dennis Underwood، نويسنده , , Shrenik K. Shah، نويسنده , , Paul E. Finke، نويسنده , , Timothy F. Miller and Daniel J. Miller، نويسنده , , Richard J. Budhu، نويسنده , , Margaret A. Cascieri، نويسنده , , Sharon Sadowski، نويسنده , , Catherine D. Strader، نويسنده ,
Abstract :
A stereocontrolled synthesis of 1-benzyloxy-2-phenylcyclohexane derivatives containing polar substituents at C3 is described. These compounds, designed to test the role of the ring nitrogen in a related series of potent piperidine-based substance P antagonists, show similar NK-1 receptor affinity, indicating that the nitrogen may serve a largely structural role in N-substituted piperidine antagonists.
