4.5 Article

Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 15, Pages 4228-4231

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.05.035

Keywords

chemokine; CCR3; pyrazolone; asthma

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The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents. (c) 2007 Elsevier Ltd. All rights reserved.

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