Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents

doi:10.1016/j.bmc.2009.05.011

	Synthesis and biological evaluation of febrifugine analogues as potential antimalarial agents
	Zhu, Shuren 2; Zhang, Quan 2; Gudise, Chandrashekar 1; Wei, Lai 2; Smith, Erika 2; Zeng, Yuling 3
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	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.