Ether derivatives 14α(Central Drug Research Institute)(Ether derivatives 14α(Central Drug Research Institute))

概要

基本信息

药物类型

小分子化药

别名-

靶点-

作用方式-

作用机制-

治疗领域

感染

在研适应症-

非在研适应症

疟疾

原研机构

Central Drug Research Institute

在研机构-

非在研机构

Central Drug Research Institute

权益机构-

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 Ether derivatives 14α(Central Drug Research Institute) 相关的临床结果

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100 项与 Ether derivatives 14α(Central Drug Research Institute) 相关的转化医学

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100 项与 Ether derivatives 14α(Central Drug Research Institute) 相关的专利（医药）

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1

项与 Ether derivatives 14α(Central Drug Research Institute) 相关的文献（医药）

2006-11-30·Journal of Medicinal Chemistry1区 · 医学

New Orally Active Derivatives of Artemisinin with High Efficacy against Multidrug-Resistant Malaria in Mice

1区 · 医学

Article

作者: Chaudhary, Sandeep ; Puri, Sunil K. ; Singh, Chandan

A new series of ether derivatives of dihydroartemisinin have been prepared and evaluated for their antimalarial activity against multidrug-resistant Plasmodium yoelii nigeriensis in mice by oral route. These new derivatives 7-17 are highly lipophilic (log P in the range of 5.51 to 7.19) as compared with beta-arteether (log P 3.84), and several of them are two- to four-fold more active than beta-arteether. Among the ether derivatives, alpha-isomers are more active than the beta-isomers. The ether derivatives 12alpha and 14alpha, the most active compounds of the series, provided 100% protection to infected mice at 12 mg/kgx4 days. In this model beta-arteether provides 100% and 20% protection at 48 mg/kgx4 days and 24 mg/kgx4 days, respectively.

100 项与 Ether derivatives 14α(Central Drug Research Institute) 相关的药物交易

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