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J Med Chem. 2011 Aug 25;54(16):5949-53. doi: 10.1021/jm200686d. Epub 2011 Jul 29.

Synthesis and antiplasmodial activity of bicyclic dioxanes as simplified dihydroplakortin analogues.

Author information

1
European Research Centre for Drug Discovery and Development (NatSynDrugs), 53100 Siena, Italy.

Abstract

Here we report the synthesis and evaluation of antiplasmodial activity of a novel series of bicyclic peroxides inspired by the marine natural compound dihydroplakortin. We developed a synthetic strategy leading to the dihydroplakortin-related peroxides in only a few steps. The in vitro antiplasmodial potency of the peroxides was similar to, or greater than, that of the reference natural compound, and structure-activity relationship studies revealed several key structural requirements for activity and potency.

PMID:
21761935
DOI:
10.1021/jm200686d
[Indexed for MEDLINE]

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