An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors

…, IM McLay, SD Pickett, AJ Collis, K Page…

Index: McKenna, Jeffrey M.; Halley, Frank; Souness, John E.; McLay, Iain M.; Pickett, Stephen D.; Collis, Alan J.; Page, Kenneth; Ahmed, Imtiaz Journal of Medicinal Chemistry, 2002 , vol. 45, # 11 p. 2173 - 2184

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Citation Number: 76

Abstract

Previously we reported the identification of RPR200765A, a potent orally bioavailable pyridine-imidazole inhibitor of p38 mitogen-activated protein (MAP) kinase which suppressed paw swelling and joint pathology in streptococcal cell wall-induced arthritis. Herein, we report the use of solid-phase combinatorial organic synthesis for the parallel processing of a related pyrimidine-imidazole-based library with two points of structural ...