Design of potent and selective 2-aminobenzimidazole-based p38α MAP kinase inhibitors with excellent in vivo efficacy

Journal of Medicinal Chemistry

Volumn 48, Issue 7, 2005, Pages 2270-2273

  De Dios, Alfonso ^a   Shih, Chuan ^b   López De Uralde, Beatriz ^a   Sánchez, Concepción ^a   Del Prado, Miriam ^a   Martín Cabrejas, Luisa M ^a   Pleite, Sehila ^a   Blanco Urgoiti, Jaime ^a   Lorite, María José ^a   Nevill Jr , C Richard ^b   Bonjouklian, Rosanne ^b   York, Jeremy ^b   Vieth, Michal ^b   Wang, Yong ^b   Magnus, Nicholas ^b   Campbell, Robert M ^b   Anderson, Bryan D ^b   McCann, Denis J ^b   Giera, Deborah D ^b   Lee, Paul A ^b   Schultz, Richard M ^b   Li, Li C ^b   Johnson, Lea M ^b   Wolos, Jeffrey A ^b   more..

^a ELI LILLY AND COMPANY   (Spain)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINOBENZIMIDAZOLE; 4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; 4 [4 (4 FLUOROPHENYL) 1 (3 PHENYLPROPYL) 5 (4 PYRIDINYL) 1H IMIDAZOL 2 YL] 3 BUTYN 1 OL; 5 (2,6 DICHLOROPHENYL) 2 (2,4 DIFLUOROPHENYLTHIO)PYRIMIDO[1,6 B]PYRIDAZIN 6 ONE; ADENOSINE TRIPHOSPHATE; BENZIMIDAZOLE DERIVATIVE; COLLAGEN; CYTOCHROME P450 3A4; DORAMAPIMOD; L 790070; MITOGEN ACTIVATED PROTEIN KINASE P38 INHIBITOR; SB 242235; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTHRITIS; ARTICLE; DRUG ACTIVITY; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME BINDING; MACROPHAGE; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTI-INFLAMMATORY AGENTS; ARTHRITIS, EXPERIMENTAL; BENZIMIDAZOLES; BINDING SITES; BIOLOGICAL AVAILABILITY; COLLAGEN; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; LIPOPOLYSACCHARIDES; MACROPHAGES, PERITONEAL; MICE; MICE, INBRED BALB C; MITOGEN-ACTIVATED PROTEIN KINASE 14; MODELS, MOLECULAR; RATS; TUMOR NECROSIS FACTOR-ALPHA;

EID: 20244384283     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm048978k     Document Type: Article

References (38)

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37. 50 is defined as the lowest dose where statistically significant efficacy was achieved, and there was at least 50% inhibition compared to vehicle control.
38. 50 was calculated from the AUC (paw swelling) or composite histology score using JMP5.1.1.