Synthesis and Antiplasmodial Activity of Bicyclic Dioxanes as Simplified Dihydroplakortin Analogues

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• 作者：Sandra Gemma ; Sanil Kunjir ; Salvatore Sanna Coccone ; Margherita Brindisi ; Vittoria Moretti ; Simone Brogi ; Ettore Novellino ; Nicoletta Basilico ; Silvia Parapini ; Donatella Taramelli ; Giuseppe Campiani ; Stefania Butini
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：August 25, 2011
• 年：2011
• 卷：54
• 期：16
• 页码：5949-5953
• 全文大小：842K
• 年卷期：v.54,no.16(August 25, 2011)
• ISSN：1520-4804

文摘

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鈥揳ctivity relationship studies revealed several key structural requirements for activity and potency.