منابع مشابه
Synthesis of a naphthyridone p38 MAP kinase inhibitor.
Compound 1 is a p38 MAP kinase inhibitor potentially useful for the treatment of rheumatoid arthritis and psoriasis. A novel six-step synthesis suitable for large-scale preparation was developed in support of a drug development program at Merck Research Laboratories. The key steps include a tandem Heck-lactamization, N-oxidation, and a highly chemoselective Grignard addition of 4-(N-tert-butylp...
متن کاملp38 MAP kinase inhibitor reverses stress-induced cardiac myocyte dysfunction.
Stress is gaining increasing acceptance as an independent risk factor contributing to adverse cardiovascular outcomes. Potential mechanisms responsible for the deleterious effects of stress on the development and progression of cardiovascular disease remain to be elucidated. An established animal model of stress in humans is the prenatally stressed (PS) rat. We stressed rats in their third trim...
متن کاملSynthesis and Evaluation of Pyridinyltriazoles as Inhibitors of p38 MAP Kinase
Objective(s) Inhibitors of p38 MAP kinase are considered as suitable target in the treatment of inflammatory diseases such as rheumatoid arthritis and bowel inflammatory diseases. The development of 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles as inhibitors of p38 MAP kinase is described. These are analogues of 4- pyridinyl imidazole p38 MAP kinase inhibitor reported by Merck Research Laborator...
متن کاملComputational investigation of ginsenoside F1 from Panax ginseng Meyer as p38 MAP Kinase Inhibitor: Molecular docking and dynamics simulations, ADMET analysis, and drug likeness prediction.
Ginsenoside F1 is a biologically active compound identified potential from Korean Panax ginseng Meyer. In the present study, the potential targets of ginsenoside F1 were investigated by computational target fishing approaches including ADMET prediction, biological activity prediction from chemical structure, molecular docking, and molecular dynamics methods. Results were suggested to express th...
متن کاملApplication of 3D-QSAR on a Series of Potent P38-MAP Kinase Inhibitors
One of the most applied methods in drug industry for development of new drugs is 3D-QSAR methodology. As p38-mitogen-activated protein kinase (p38-MAPK) plays a crucial role in regulating the production of such proinflammatory cytokines as tumor necrosis factor-α (TNF-α) and interleukin-1, emerging as an attractive target for new anti-inflammatory agents, we used a 3D-QSAR based method of Compa...
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ژورنال
عنوان ژورنال: Japanese Journal of Clinical Immunology
سال: 2007
ISSN: 0911-4300,1349-7413
DOI: 10.2177/jsci.30.390