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Merck
  • Antimalarials based on the dioxane scaffold of plakortin. A concise synthesis and SAR studies.

Antimalarials based on the dioxane scaffold of plakortin. A concise synthesis and SAR studies.

Bioorganic & medicinal chemistry (2010-12-03)
Caterina Fattorusso, Marco Persico, Nicoletta Basilico, Donatella Taramelli, Ernesto Fattorusso, Fernando Scala, Orazio Taglialatela-Scafati
要旨

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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ブランド
製品内容

Sigma-Aldrich
trans-2-ノネナール, 97%