Design and synthesis of endoperoxide antimalarial prodrug models

被引：51

作者：

O'Neill, PM ^{[1
]}

Stocks, PA

Pugh, MD

Araujo, NC

Korshin, EE

Bickley, JF

Ward, SA

Bray, PG

Pasini, E

Davies, J

Verissimo, E

Bachi, MD

机构：

[1] Univ Liverpool, Robert Robinson Labs, Dept Chem, Liverpool L69 7ZD, Merseyside, England

[2] Weizmann Inst Sci, Dept Organ Chem, IL-76100 Rehovot, Israel

[3] Univ Liverpool Liverpool Sch Trop Med, Liverpool L3 5QA, Merseyside, England

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2004年 / 43卷 / 32期

关键词：

antimalarial agents; chalcones; combination chemotherapy; cysteine protease inhibitors; endoperocides;

D O I：

10.1002/anie.200453859

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A masked combination chemotherapy which relies on the embedding of a number of active components, in a latent form, within a single endoperoxidic chemical entity is the aim of the research presented. The approach is illustrated by means of purposely designed bicyclic endoperoxide prodrug prototypes 1 and subsequently validated through the study of model compounds 2 (Ar= Ph, p-FC 6H4, p-ClC6H4.

引用

页码：4193 / 4197

页数：5

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