M N Agafonova, O S Vasileva, E M Fafanova, D J Grishaev, M N Sarynin, M V Pugachev, Yu G Shtyrlin
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引用次数: 0
Abstract
Prodrugs based on pyridoxine and ketorolac (the most potent analgesic NSAIDs) exhibit analgesic activity comparable to ketorolac in vivo and significantly higher safety and prolonged action. In this study the antioxidant and protective properties, inhibitory activity against cyclooxygenase (COX) and intracellular permeability for two prodrug bipharmacophoric conjugates based on pyridoxine and ketorolac have been investigated in vitro. Their inhibitory activity towards the COX-1 and COX-2 enzymes was comparable to that of ketorolac (the IC50 values ranged from 12.0 μM to 34.7 μM). These compounds markedly protected albumin against thermal and chemical (urea and citric acid) treatments and demonstrated the cell-penetrating ability through passive diffusion.
Biomeditsinskaya khimiyaBiochemistry, Genetics and Molecular Biology-Biochemistry, Genetics and Molecular Biology (all)
CiteScore
1.30
自引率
0.00%
发文量
49
期刊介绍：
The aim of the Russian-language journal "Biomeditsinskaya Khimiya" (Biomedical Chemistry) is to introduce the latest results obtained by scientists from Russia and other Republics of the Former Soviet Union. The Journal will cover all major areas of Biomedical chemistry, including neurochemistry, clinical chemistry, molecular biology of pathological processes, gene therapy, development of new drugs and their biochemical pharmacology, introduction and advertisement of new (biochemical) methods into experimental and clinical medicine etc. The Journal also publish review articles. All issues of journal usually contain invited reviews. Papers written in Russian contain abstract (in English).
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