- 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
PMID21123074
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.
材料