4.5 Article

Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 1, Pages 288-293

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.015

Keywords

MK-7246; CRTH2 antagonist; DP2 antagonist; Asthma; Respiratory diseases

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In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two synthetic sequences enabling the preparation of this novel class of CRTH2 antagonist are reported. Finally, the pharmacokinetic and metabolic profile of MK-7246 is disclosed. (C) 2010 Elsevier Ltd. All rights reserved.

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