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

Porter, David, Bradley, Michelle, Brown, Zarin, Charlton, Steven, Cox, Brian, Hunt, Peter, Janus, Diana, Lewis, Sarah, Oakley, Paul, O'Connor, Des, Reilly, John, 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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