Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents | |
Zhu, Shuren2; Zhang, Quan2; Gudise, Chandrashekar1; Wei, Lai2; Smith, Erika2; Zeng, Yuling3 | |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
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2009-07-01 | |
卷号 | 17期号:13页码:4496-4502 |
关键词 | Antimalarial Febrifugine |
ISSN号 | 0968-0896 |
DOI | 10.1016/j.bmc.2009.05.011 |
文献子类 | Article |
英文摘要 | Febrifugine is an alkaloid isolated from Dichroa febrifuga Lour as the active component against Plasmodium falciparum. Adverse side effects have precluded febrifugine as a potential clinical drug. In this study novel febrifugine analogues were designed and synthesized. Lower toxicity was achieved by reducing or eliminating the tendency of forming chemically reactive and toxic intermediates and metabolites. Synthesized compounds were evaluated for acute toxicity and in vitro and in vivo antimalarial efficacy. Some compounds are much less toxic than the natural product febrifugine and existing antimalarial drug chloroquine and are expected to possess wide therapeutic windows. These compounds, as well as the underlying design rationale, may find usefulness in the discovery and development of new antimalarial drugs. (C) 2009 Elsevier Ltd. All rights reserved. |
资助项目 | National Institutes of Health[R43 AI077109] |
WOS关键词 | PLASMODIUM MALARIA PARASITE ; FALCIPARUM ; INVITRO |
WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
语种 | 英语 |
出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
WOS记录号 | WOS:000266822900025 |
内容类型 | 期刊论文 |
源URL | [http://119.78.100.183/handle/2S10ELR8/279194] ![]() |
专题 | 中国科学院上海药物研究所 |
通讯作者 | Zhu, Shuren |
作者单位 | 1.Indian Inst Chem Technol, Hyderabad 500007, Andhra Pradesh, India; 2.Radix Pharmaceut Inc, Potomac, MD 20854 USA; 3.Chinese Acad Sci, Inst Mat Med, Shanghai 201203, Peoples R China |
推荐引用方式 GB/T 7714 | Zhu, Shuren,Zhang, Quan,Gudise, Chandrashekar,et al. Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2009,17(13):4496-4502. |
APA | Zhu, Shuren,Zhang, Quan,Gudise, Chandrashekar,Wei, Lai,Smith, Erika,&Zeng, Yuling.(2009).Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents.BIOORGANIC & MEDICINAL CHEMISTRY,17(13),4496-4502. |
MLA | Zhu, Shuren,et al."Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents".BIOORGANIC & MEDICINAL CHEMISTRY 17.13(2009):4496-4502. |
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