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Synthesis of New 1,2,4-Trioxanes and their Antimalarial Activity

✍ Scribed by Charles W. Jefford; Ernest C. McGoran; John Boukouvalas; Geoffrey Richardson; Brian L. Robinson; Wallace Peters

Publisher: John Wiley and Sons
Year: 1988
Tongue: German
Weight: 497 KB
Volume: 71
Category: Article
ISSN: 0018-019X
DOI: 10.1002/hlca.19880710722

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✦ Synopsis

The three dihydronaphtho[l,2,4]trioxines e l l have been synthesized and two of them converted to the five carbamate and ester derivatives 12-16 (Schemes I and 2). The resulting new trioxanes together with two already known and ascaridole (7) were tested for antimalarial activity against the sensitive N strain of Plasmodium berghei in mice. On comparison with artemisinin (1) and dihydroartemisinin (2), modest activity was found. The four most active compounds were some 12-18 times less potent than 1. ') Artemisinin is also known as arteannuin and qinghaosu (QHS).

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