Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 21, Pages 6582-6591Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.08.025
Keywords
CRTh2 receptor antagonist; Allergy
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Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development. (C) 2013 Elsevier Ltd. All rights reserved.
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