Author/Authors :
Roland L. Knight، نويسنده , , Daniel R. Allen، نويسنده , , Helen L. Birch، نويسنده , , Gayle A. Chapman، نويسنده , , Frances C. Galvin، نويسنده , , Louise A. Jopling، نويسنده , , Christopher J. Lock، نويسنده , , Johannes W.G. Meissner، نويسنده , , David A. Owen، نويسنده , , Gilles Raphy، نويسنده , , Robert J. Watson، نويسنده , , Sophie C. Williams، نويسنده ,
Abstract :
The synthesis and biological evaluation of a novel series of 2-aminoquinoline substituted piperidines and tropanes incorporating a homotropene moiety is herein described. The series exhibits potent antagonism of the CXCR3 receptor and superior physicochemical properties. Compound 24d was found to be orally bioavailable, and PK/PD studies suggested it as a suitable tool for studying the role of CXCR3 in models of disease.
Keywords :
CXCR3 , Quinoline , Tool reagent , tropane , Chemokine , inflammation
