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Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis

Miltz, Wolfgang and Velcicky, Juraj and Dawson King, Janet and Littlewood-Evans, Amanda and Ludwig, Marie-Gabrielle and Seuwen, Klaus and Feifel, Roland and Oberhauser, Berndt and Meyer, Arndt and Gabriel, Daniela and Loetscher, Pius (2017) Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis. Bioorganic & Medicinal Chemistry, 25 (16). pp. 4512-4525. ISSN 0968-0896

Abstract

The G-protein-coupled receptor GPR4 functions as a proton sensor activated by extracellular acidic pH and has been implicated in playing a key role in acidosis associated with a variety of inflammatory conditions. A selective GPR4 antagonist 2 was developed, starting from a high throughput screening hit 1. The compound showed potent cellular activity and was efficacious in animal models of angiogenesis, inflammation, and pain.

Item Type: Article
Keywords: GPR4; Amino-pyrimidine derivatives; Imidazo-pyridine derivatives; Angiogenesis; Inflammation; Pain
Date Deposited: 09 Aug 2017 00:45
Last Modified: 09 Aug 2017 00:45
URI: https://oak.novartis.com/id/eprint/31037

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