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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 and Medicinal Chemistry, 25 (16). pp. 4512-4525. ISSN 14643391

Abstract

GPR4, a G-protein coupled receptor, functions as a proton sensor being activated by extracellular acidic pH and has been implicated in playing a key role in acidosis associated with a variety of inflammatory conditions. An orally active GPR4 antagonist 39c was developed, starting from a high throughput screening hit 1. The compound shows potent cellular activity and is efficacious in animal models of angiogenesis, inflammation and pain.

Item Type: Article
Keywords: Amino-pyrimidine derivatives Angiogenesis GPR4 Imidazo-pyridine derivatives Inflammation Pain
Date Deposited: 20 Dec 2017 00:45
Last Modified: 25 Jan 2019 00:45
URI: https://oak.novartis.com/id/eprint/32976

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