Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 21, Pages 5118-5122Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.09.005
Keywords
CRTh2 antagonist; Receptor residence time; Structure-activity relationship (SAR); Structure-kinetic relationship (SKR)
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A knowledge-based design strategy led to the discovery of several new series of potent and orally bio-available CRTh2 antagonists where a bicyclic heteroaromatic ring serves as the central core. Structure-kinetic relationships (SKR) opened up the possibility of long receptor residence times. (C) 2014 Elsevier Ltd. All rights reserved.
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