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Page 1: Hit-to-Lead Studies: The Discovery of Potent, Orally Bioavailable Thiazolopyrimidine CXCR2 Receptor Antagonists

2006

Fused pyrimidine derivativesR 0515 Hit-to-Lead Studies: The Discovery of Potent, Orally Bioavailable Thiazolopyri-

midine CXCR2 Receptor Antagonists. — A hit-to-lead optimization program on the high throughput screening hit (Ia) results in the discovery of potent CXCR2 receptor antagonist (Ic). — (BAXTER*, A.; COOPER, A.; KINCHIN, E.; MOAKES, K.; UNITT, J.; WALLACE, A.; Bioorg. Med. Chem. Lett. 16 (2006) 4, 960-963; AstraZeneca R&D Charnwood, Loughborough, Leicestershire LE11 5RH, UK; Eng.) — D. Singer

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