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Antimalarials based on the dioxane scaffold of plakortin. A concise synthesis and SAR studies by Caterina Fattorusso; Marco Persico; Nicoletta Basilico; Donatella Taramelli; Ernesto Fattorusso; Fernando Scala; Orazio Taglialatela-Scafati is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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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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Author

Caterina Fattorusso; Marco Persico; Nicoletta Basilico; Donatella Taramelli; Ernesto Fattorusso; Fernando Scala; Orazio Taglialatela-Scafati

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2011

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)