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Iranian Journal of Basic Medical Sciences، جلد ۱۵، شماره ۴، صفحات ۹۴۵-۹۵۰
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| عنوان انگلیسی |
Synthesis and Evaluation of Pyridinyltriazoles as Inhibitors of p38 MAP Kinase |
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| چکیده انگلیسی مقاله |
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 Laboratories, in which imidazole ring has been replaced with triazole. Materials and Methods Reaction of pyridine-4-carboxylic acid hydrazide 1 and arylisothiocyanate (2a, b) gave the intermediate thiourea derivative 3a, b (Figure 2). Refluxing of the latter in aqueous saturated sodium carbonate gave 1-aryl-5-mercapto-2-(4-pyridinyl) triazoles 4a, b. Treatment of 4a, b with alkyl iodide afforded the desired 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles (5a-d). P38 MAP kinase inhibitory activity of the synthesized compounds was evaluated in vitro by ELISA method and also by molecular docking. Results Compound 5c at 1 µM concentration and compound 5d at 1 µM and 10 µM significantly inhibited the p38 phosphorylation. These inhibitory effects are equal to those of standard compound SB202190 and no significant differences were observed. Conclusion We demonstrated that both tested compounds have inhibitory effect on p38 MAP kinase and we did not find significant difference between their inhibitory effects and those of standard inhibitor SB202190. |
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| کلیدواژه‌های انگلیسی مقاله |
Inhibitors, p38 MAP kinase, Pyridinylimidazoles |
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| نویسندگان مقاله |
سید عادل معلم | seyed adel moallem
pharmaceutical sciences research centre, mashhad university of medical sciences mashhad, iran|medical toxicology research centre, mashhad university of medical sciences mashhad, iran|school of pharmacy, mashhad university of medical sciences mashhad, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی مشهد (Mashhad university of medical sciences)
فرزین هادی زاده | farzin hadizadeh
biotechnology research centre, mashhad university of medical sciences, mashhad, iran|school of pharmacy, mashhad university of medical sciences mashhad, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی مشهد (Mashhad university of medical sciences)
فاطمه عبدل آبادی | fatemeh abdol abadi
medical toxicology research centre, mashhad university of medical sciences mashhad, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی مشهد (Mashhad university of medical sciences)
محمود شهرکی | mahmoud shahraki
school of pharmacy, mashhad university of medical sciences mashhad, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی مشهد (Mashhad university of medical sciences)
جمال شمس آرا | jamal shamsara
school of pharmacy, mashhad university of medical sciences mashhad, iran
سازمان اصلی تایید شده: دانشگاه علوم پزشکی مشهد (Mashhad university of medical sciences)
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| نشانی اینترنتی |
http://ijbms.mums.ac.ir/article_4883.html |
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| کد مقاله (doi) |
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| زبان مقاله منتشر شده |
en |
| موضوعات مقاله منتشر شده |
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| نوع مقاله منتشر شده |
Original Article |
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