Towards the improvement of the synthesis of novel 4(5)-aryl-5(4)-heteroaryl-2-thio-substituted imidazoles and their p38 MAP kinase inhibitory activity.
نویسندگان
چکیده
A series of 2-alkylsulfanyl-4-(4-fluorophenyl)-5-(2-aminopyridin-4-yl)-substituted imidazoles was prepared and interaction possibilities of the 2-thioether moiety with phosphate/ribose binding pockets of p38 MAP kinase were investigated. Introduction of the alkyl/benzyl amino function at the pyridine moiety was carried out via nucleophilic substitution or via palladium catalyzed aryl-C-N-bond formation.
منابع مشابه
Synthesis 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 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...
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Nano TiO2 supported on SiO2 (Nano TiO2@SiO2) as a solid Lewis acid, was described to be an effective and reusable catalyst for one-pot three-component reaction of benzil, aryl aldehydes and ammonium acetate for the synthesis 2-aryl-4,5-diphenyl-1H-imdazoles synthesis. To explore the high efficacy of the catalytic system the four-component cyclization of benzil, aryl aldehydes, ammonium acetate ...
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ورودعنوان ژورنال:
- Organic & biomolecular chemistry
دوره 6 3 شماره
صفحات -
تاریخ انتشار 2008