European Research Center for Drug Discovery and Development NatSynDrugs

Siena, Italy

European Research Center for Drug Discovery and Development NatSynDrugs

Siena, Italy
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Gemma S.,European Research Center for Drug Discovery and Development NatSynDrugs | Gemma S.,University of Siena | Gemma S.,University of Turin | Kunjir S.,European Research Center for Drug Discovery and Development NatSynDrugs | And 31 more authors.
Journal of Medicinal Chemistry | Year: 2011

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. © 2011 American Chemical Society.


PubMed | European Research Center for Drug Discovery and Development NatSynDrugs
Type: Journal Article | Journal: Journal of medicinal chemistry | Year: 2011

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.

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