Antiplasmodial activity of alkyl-substituted 1,2-dioxetanes against Plasmodium falciparum

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• 作者：Adriana F. Silva^a ; Vani X. Oliveira Jr.^a ; Leandro S. Silva^b ; Ana A.S. Pinheiro^b ; Luiz F.M.L. Ciscato^a ; ^{luiz.ciscato@ufabc.edu.br" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Antimalarials ; Peroxides ; 1 ; 2-Dioxetane
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 October 2016
• 年：2016
• 卷：26
• 期：20
• 页码：5007-5008
• 全文大小：301 K

文摘

This article reports the in vitro antiplasmodial activity of two endoperoxides of the class 1,2-dioxetanes against Plasmodium falciparum: bis(adamantyl)-1,2-dioxetane and 3,3,4,4-tetramethyl-1,2-dioxetane. The results reveal that bis(adamantyl)-1,2-dioxetane displays substantial antiplasmodial activity, at least two orders of magnitude higher than that of artemisinin, while 3,3,4,4-tetramethyl-1,2-dioxetane is less active.