Pyrimidinylimidazole inhibitors of CSBP/P38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 22, 1998, Pages 3111-3116

  Adams, Jerry L ^a   Boehm, Jeffrey C ^a   Kassis, Shouki ^a   Gorycki, Peter D ^a   Webb, Edward F ^a   Hall, Ralph ^a   Sorenson, Margaret ^a   Lee, John C ^a   Ayrton, Andrew ^a   Griswold, Don E ^a   Gallagher, Timothy F ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; 5 (4 PYRIDINYL) 4 (4 FLUOROPHENYL) 1 (3 MORPHOLINOPROPYL)IMIDAZOLE; 6 (4 FLUOROPHENYL) 2,3 DIHYDRO 5 (4 PYRIDYL)IMIDAZO[2,1 B]THIAZOLE; CYTOCHROME P450; IMIDAZOLE DERIVATIVE; MITOGEN ACTIVATED PROTEIN KINASE; PYRIMIDINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; DRUG ACTIVITY; ENZYME INHIBITION; INFLAMMATION; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

EID: 0032541986     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00549-6     Document Type: Article

References (19)

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19. 15. Not included in Table 2 is compound 4c, which failed to demonstrate statistically significant activity in the mouse LPS-induced TNF assay when dosed orally at 50 mg/kg (12% inhibiton). Additional compounds tested in the mouse model at a dose of 50 mg/kg were 4j (21% inh.), 41 (37% inh.) and 4m (33% inh).