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The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists
journal contribution
posted on 2023-06-08, 19:29 authored by David W Porter, Michelle Bradley, Zarin Brown, Steven J Charlton, Brian Cox, Peter Hunt, Diana Janus, Sarah Lewis, Paul Oakley, Des O'Connor, John Reilly, Nichola Smith, Neil J PressA 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.
History
Publication status
- Published
Journal
Bioorganic and Medicinal Chemistry LettersISSN
0960-894XPublisher
ElsevierExternal DOI
Issue
15Volume
24Page range
3285-3290Department affiliated with
- Chemistry Publications
Full text available
- No
Peer reviewed?
- Yes
Legacy Posted Date
2015-01-12Usage metrics
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