Synthesis and evaluation of 4-quinazolinone compounds as potential antimalarial agents

	Synthesis and evaluation of 4-quinazolinone compounds as potential antimalarial agents
	Zhu, SR; Wang, J; Chandrashekar, G; Smith, E; Liu, XJ; Zhang, YS
刊名	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
	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
内容类型	期刊论文
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.