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The Discovery of Potent, Orally Bioavailable Pyrimidine-5-carbonitrile-6-alkyl CXCR2 Receptor Antagonists.

Porter, David and Bradley, Michelle and Brown, Zarin and Charlton, Steven and Cox, Brian and Hunt, Peter and Janus, Diana and Lewis, Sarah and Oakley, Paul and O'Connor, Des and Reilly, John and Smith, Nichola and Press, Neil (2014) The Discovery of Potent, Orally Bioavailable Pyrimidine-5-carbonitrile-6-alkyl CXCR2 Receptor Antagonists. Biorganic & Medicinal Chemistry Letters.

Abstract

A Hit-to-Lead optimisation programme was carried out on the Novartis archive screening hit, pyrimidine 2-((2,6-dichlorobenzyl)thio)-5-isocyano-6-phenylpyrimidin-4-ol 4, resulting in the discovery of CXCR2 receptor antagonist 2-((2,3-difluorobenzyl)thio)-6-(2-(hydroxymethyl)cyclopropyl)-5-isocyanopyrimidin-4-ol 24. The SAR was investigated by systematic variation of the aromatic group at c-6, the linker between c-2 and the halogenated ring and the c-5 nitrile moiety.

Item Type: Article
Keywords: CXCR2
Date Deposited: 13 Oct 2015 13:13
Last Modified: 13 Oct 2015 13:13
URI: https://oak.novartis.com/id/eprint/20993

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