Antimalarials based on the dioxane scaffold of plakortin. A concise synthesis and SAR studies |
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Authors: | Fattorusso Caterina Persico Marco Basilico Nicoletta Taramelli Donatella Fattorusso Ernesto Scala Fernando Taglialatela-Scafati Orazio |
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Affiliation: | a Dipartimento di Chimica delle Sostanze Naturali, Università di Napoli ‘Federico II’, Via D. Montesano, 49, I-80131 Napoli, Italy b Dipartimento di Sanità Pubblica-Microbiologia-Virologia, Università degli Studi di Milano, Via Pascal, 36 Milano, Italy |
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Abstract: | In our search for new antimalarial agents inspired by natural products, we describe herein the synthesis, the evaluation of in vitro antiplasmodial activity, and the SAR studies for a series of endoperoxide antimalarials based on the plakortin scaffold. These simplified analogues are characterized by: (i) a 3,6-dihydro-1,2-dioxin ring or a 1,2-dioxane ring disubstituted at C-4 and C-5; (ii) a pentyl substituent at C-6 (‘western’ alkyl side chain) and they have been prepared from commercially available material using simple reactions. |
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Keywords: | Antimalarial Endoperoxide Plakortin Knoevenagel reaction Photooxygenation |
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