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  • Title: The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists.
    Author: Porter DW, Bradley M, Brown Z, Charlton SJ, Cox B, Hunt P, Janus D, Lewis S, Oakley P, O'Connor D, Reilly J, Smith N, Press NJ.
    Journal: Bioorg Med Chem Lett; 2014 Aug 01; 24(15):3285-90. PubMed ID: 24974342.
    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.
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