Development of CXCR3 antagonists. Part 4: Discovery of 2-amino-(4-tropinyl) quinolines

…, JWG Meissner, DA Owen, G Raphy, RJ Watson…

Index: Knight, Roland L.; Allen, Daniel R.; Birch, Helen L.; Chapman, Gayle A.; Galvin, Frances C.; Jopling, Louise A.; Lock, Christopher J.; Meissner, Johannes W.G.; Owen, David A.; Raphy, Gilles; Watson, Robert J.; Williams, Sophie C. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 2 p. 629 - 633

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Citation Number: 28

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.