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Synthesis and antimalarial activity of artemisinin derivatives containing an amino group.

Abstract：

:In search of water-soluble artemisinin derivatives that are more stable than sodium artesunate, over 30 derivatives containing an amino group (compounds 3-5) were synthesized and tested in mice. All products tested (except 5a and 5b) are the beta isomers. These basic compounds combined with organic acids (oxalic acid, maleic acid, etc. ) to yield the corresponding salts. Generally, the maleates have better solubility in water than the corresponding oxalates. The aqueous solutions of these salts can be kept at room temperature for several weeks without any discernible decomposition. Compounds 3f, 3h, and 3r are much more active against P. berghei than artesunic acid by oral administration and therefore were further tested in monkeys. However, their oral efficacies are poorer than that of artesunic acid against P. knowlesi in rhesus monkeys. It is interesting to note that 3f, 3h, and 3r showed much lower efficacies against P. berghei when they were administered subcutaneously than orally.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Li Y,Zhu YM,Jiang HJ,Pan JP,Wu GS,Wu JM,Shi YL,Yang JD,Wu BA

doi

10.1021/jm990552w

keywords:

subject

Has Abstract

pub_date

2000-04-20 00:00:00

pages

1635-40

issue

8

eissn

0022-2623

issn

1520-4804

pii

jm990552w

journal_volume

43

pub_type

杂志文章

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