Synthesis and evaluation of naphthyridine compounds as antimalarial agents

doi:10.1016/j.bmc1.2007.09.044

	Synthesis and evaluation of naphthyridine compounds as antimalarial agents
	Zhu, Shuren ; Zhang, Quart ; Gudise, Chandrashekar ; Meng, Li ; Wei, Lai ; Smith, Erika ; Kong, Yuhang
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2007-11-15
卷号	17 期号:22 页码:6101-6106
关键词	primaquine antimalarial
ISSN号	0960-894X
DOI	10.1016/j.bmc1.2007.09.044
文献子类	Article
英文摘要	Primaquine is the drug of choice for the radical cure of Plasmodium vivax malaria, but possesses serious side effects. In this study novel primaquine analogues were designed and synthesized. Lower toxicity was achieved by reducing or eliminating the tendency of forming chemically reactive and toxic intermediates and metabolites. In vitro and in vivo studies found that synthesized compounds were less toxic than the parent compound primaquine, while preserving the desired antimalarial activity. Some of these compounds possess a therapeutic index over 10 times superior to that of 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) 2007 Elsevier Ltd. All rights reserved.
资助项目	NIAID NIH HHS[R44 AI063734-02] ; NIAID NIH HHS[R44 AI 063734] ; NIAID NIH HHS[R44 AI063734]
WOS关键词	INDUCED HEMOLYTIC-ANEMIA ; PLASMODIUM-FALCIPARUM ; METHEMOGLOBIN TOXICITY ; PUTATIVE METABOLITES ; PRIMAQUINE ; INVITRO ; BLOOD ; SUSCEPTIBILITY ; GLUTATHIONE ; DERIVATIVES
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000250906200010
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/273111]
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.Chinese Acad Sci, Inst Mat Med, Shanghai 201203, Peoples R China 2.Radix Pharmaceut Inc, Rockville, MD 20850 USA 3.Indian Inst Chem Technol, Hyderabad 500007, Andhra Pradesh, India
推荐引用方式 GB/T 7714	Zhu, Shuren,Zhang, Quart,Gudise, Chandrashekar,et al. Synthesis and evaluation of naphthyridine compounds as antimalarial agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2007,17(22):6101-6106.
APA	Zhu, Shuren.,Zhang, Quart.,Gudise, Chandrashekar.,Meng, Li.,Wei, Lai.,...&Kong, Yuhang.(2007).Synthesis and evaluation of naphthyridine compounds as antimalarial agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,17(22),6101-6106.
MLA	Zhu, Shuren,et al."Synthesis and evaluation of naphthyridine compounds as antimalarial agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 17.22(2007):6101-6106.