Antimalarial peroxides: The first intramolecular 1,2,4,5-tetraoxane

Abstract

An intramolecular steroidal 1,2,4,5-tetraoxane has been synthesised in six steps starting from methyl3-oxo-7α,12α-diacetoxy-5β-cholan-24-oate. The synthesised 1,2,4,5-tetraoxane has moderate in vitro antimalarial activity against P. falciparum strains (IC50 (D6) = 0.35 µg/mL; IC50 (W2) = 0.29 µg/mL).

Polazeći od methyl 3-oxo-7α,12α-diacetoxy-5β-cholan-24-oate sintetisan je u šest faza intramolekulski steroidni 1,2,4,5-tetraoksan. Proizvod ima umerenu in vitro antimalarijsku aktivnost prema P. falciparum sojevima (IC50 (D6) = 0.35 µg/mL; IC50 (W2) = 0.29 µg/mL).