Title of article
Development of CXCR3 antagonists. Part 4: Discovery of 2-amino-(4-tropinyl)quinolines
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
629
To page
633
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799028
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