Synthesis and evaluation of 4-quinazolinone compounds as potential antimalarial agents
文献类型：期刊论文
| 作者 | Zhu, SR; Wang, J; Chandrashekar, G; Smith, E; Liu, XJ; Zhang, YS |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2010 |
| 卷号 | 45期号:9页码:3864-3869 |
| 关键词 | Drug design Febrifugine Malaria chemotherapy Plasmodium falciparum |
| 通讯作者 | Zhu, SR (reprint author), Radix Pharmaceut Inc, 13303 Sunny Brooke PL,Rm 101, Potomac, MD 20854 USA.,shuren.zhu@gmail.com |
| 英文摘要 | Febrifugine is an alkaloid isolated from Dichroa febrifuga as the active component against Plasmodium falciparum. Adverse side effects have precluded febrifugine as a potential clinical drug. As part of an ongoing malaria chemotherapy project, novel febrifugine analogues were designed and synthesized. Lower toxicity of these newly designed compounds was achieved by reducing or eliminating the tendency to form chemically reactive and toxic intermediates. New compounds possess excellent in vivo antimalarial activity and most of them become less toxic than the natural product febrifugine. Some of the compounds possess a therapeutic index over ten times superior to that of febrifugine and the commonly used antimalarial drug chloroquine. These compounds, as well as the underlying design rationale, may find usefulness in the discovery and development of new antimalarial drugs. (C) 2010 Elsevier Masson SAS. All rights reserved. |
| 学科主题 | Pharmacology & Pharmacy |
| 类目[WOS] | Chemistry, Medicinal |
| 关键词[WOS] | PLASMODIUM MALARIA PARASITE ; FEBRIFUGINE ANALOGS ; ORGANIC-SYNTHESIS ; FALCIPARUM ; INVITRO |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000281568600042 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/1048]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 推荐引用方式 GB/T 7714 | Zhu, SR,Wang, J,Chandrashekar, G,et al. Synthesis and evaluation of 4-quinazolinone compounds as potential antimalarial agents[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2010,45(9):3864-3869. |
| APA | Zhu, SR,Wang, J,Chandrashekar, G,Smith, E,Liu, XJ,&Zhang, YS.(2010).Synthesis and evaluation of 4-quinazolinone compounds as potential antimalarial agents.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,45(9),3864-3869. |
| MLA | Zhu, SR,et al."Synthesis and evaluation of 4-quinazolinone compounds as potential antimalarial agents".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 45.9(2010):3864-3869. |
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