Porter, David W, Bradley, Michelle, Brown, Zarin, Charlton, Steven J, Cox, Brian, Hunt, Peter, Janus, Diana, Lewis, Sarah, Oakley, Paul, O'Connor, Des, Reilly, John, Smith, Nichola and Press, Neil J (2014) The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 24 (15). pp. 3285-3290. ISSN 0960-894X

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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
Schools and Departments:	School of Life Sciences > Chemistry
Subjects:	Q Science > QD Chemistry
Depositing User:	Tom Gittoes
Date Deposited:	12 Jan 2015 11:20
Last Modified:	26 Jan 2018 12:58
URI:	http://srodev.sussex.ac.uk/id/eprint/52035

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