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学科主题: 生命有机化学 ; 氟化学
题名: Methyl-monofluorination of ibuprofen selectively increases its inhibitory activity toward cyclooxygenase-1 leading to enhanced analgesic activity and reduced gastric damage in vivo
其他题名: 甲基-单氟代布洛芬选择性增强对Cyclooxygenase-1的抑制所导致的体内的止痛能力增强和胃受损降低
作者: Su H(苏红) ; Xie YL(谢雨礼) ; Liu WB(刘文博) ; You SL(游书力)
通讯作者: 谢雨礼 ; 游书力
刊名: Bioorg. Med. Chem. Lett.
发表日期: 2011
卷: 21, 期:12, 页:3578-3582
收录类别: SCI
部门归属: 上海海尼药业有限公司; 中科院上海有机化学研究所
英文摘要: Newly developed monofluoromethylation reaction provided access to various bioactive molecules with an interesting monofluoromethyl unit. An iridium-catalyzed asymmetric version was employed for large-scale methyl-monofluorination of widely used nonsteroidal anti-inflammatory drug ibuprofen (the active S isoform). The methyl-monofluorinated ibuprofen was found to selectively inhibit cyclooxygenase-1 over cyclooxygenase-2 and surprisingly, the compound, with almost equal pharmacokinetic profile, was shown to increase analgesic activity and diminish gastric damage in animal models comparing to the parent drug ibuprofen. Therefore, methyl-monofluorination could be a useful strategy for improving efficacy and safety profile of drugs from the 'profen' family. (C) 2011 Elsevier Ltd. All rights reserved.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000291145900015
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/22530
Appears in Collections:金属有机化学国家重点实验室_期刊论文

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Recommended Citation:
Su H,Xie YL,Liu WB,et al. Methyl-monofluorination of ibuprofen selectively increases its inhibitory activity toward cyclooxygenase-1 leading to enhanced analgesic activity and reduced gastric damage in vivo[J]. Bioorg. Med. Chem. Lett.,2011,21(12):3578-3582.
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