Methyl-monofluorination of ibuprofen selectively increases its inhibitory activity toward cyclooxygenase-1 leading to enhanced analgesic activity and reduced gastric damage in vivo
文献类型：期刊论文
| 作者 | Su H(苏红) ; Xie YL(谢雨礼) ; Liu WB(刘文博) ; You SL(游书力) |
| 刊名 | Bioorg. Med. Chem. Lett.
 |
| 出版日期 | 2011 |
| 卷号 | 21期号:12页码:3578-3582 |
| ISSN号 | 0960-894X |
| 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 |
| 通讯作者 | 谢雨礼 ; 游书力 |
| 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. |
| 学科主题 | 生命有机化学 ; 氟化学 |
| 收录类别 | SCI |
| 原文出处 | http://dx.doi.org/10.1016/j.bmcl.2011.04.114 |
| 语种 | 英语 |
| WOS记录号 | WOS:000291145900015 |
| 公开日期 | 2013-03-04 |
| 源URL | [http://202.127.28.38/handle/331003/22530]  |
| 专题 | 上海有机化学研究所_金属有机化学国家重点实验室 |
| 推荐引用方式 GB/T 7714 | 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. |
| APA | 苏红,谢雨礼,刘文博,&游书力.(2011).Methyl-monofluorination of ibuprofen selectively increases its inhibitory activity toward cyclooxygenase-1 leading to enhanced analgesic activity and reduced gastric damage in vivo.Bioorg. Med. Chem. Lett.,21(12),3578-3582. |
| MLA | 苏红,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".Bioorg. Med. Chem. Lett. 21.12(2011):3578-3582. |
入库方式： OAI收割
来源：上海有机化学研究所
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