SYNTHESIS AND ANTIMALARIAL EVALUATION OF 2,3,5-TRIOXABICYCLO[2.2.2]OCTANES, MODELS FOR THE PUTATIVE PHARMACOPHORE OF QINGHAOSU (ARTEMISININ)

被引：6

作者：

CASTEEL, DA

JUNG, KE

GERENA, L

MILHOUS, W

机构：

[1] Division of Medicinal and Natural Products Chemistry, College of Pharmacy, University of Iowa, Iowa City

[2] Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(01)81211-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Hydroperoxy-2-methoxytetrahydropyrans are cyclized with transacetalization in the presence of Amberlyst-15 and molecular sieves to 2,3,5-trioxabicyclo[2.2.2]octanes. models of the proposed pharmacophore of qirighaosu. These bridged bicyclic trioxanes exhibit only marginal antimalarial activity.

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页码：623 / 626

页数：4

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