1-2-4-trioxane has been researched along with allyl-alcohol* in 2 studies
2 other study(ies) available for 1-2-4-trioxane and allyl-alcohol
| Article | Year |
|---|---|
Synthesis, in vitro and in vivo antimalarial assessment of sulfide, sulfone and vinyl amide-substituted 1,2,4-trioxanes prepared via thiol-olefin co-oxygenation (TOCO) of allylic alcohols.
Thiol-Olefin Co-Oxygenation (TOCO) methodology has been applied to the synthesis of a small library of weak base and polar 1,2,4-trioxanes. The 1,2,4-trioxane units synthesised exhibit remarkable stability as they survive base catalysed hydrolysis and mixed anhydride/amine coupling reactions. This unique stability feature has enabled a range of novel substitution patterns to be incorporated within the spiro 1,2,4-trioxane unit. Selected analogues express potent in vitro nM antimalarial activity, low cytotoxicity and oral activity in the Plasmodium berghei mouse model of malaria. Topics: Alkenes; Amides; Animals; Antimalarials; Crystallography, X-Ray; Disease Models, Animal; Heterocyclic Compounds; Malaria; Mice; Models, Molecular; Molecular Structure; Oxidation-Reduction; Oxygen; Parasitic Sensitivity Tests; Plasmodium berghei; Propanols; Stereoisomerism; Sulfhydryl Compounds; Sulfides; Sulfones | 2010 |
New functionalized 1,2,4-trioxepanes: synthesis and antimalarial activity against multi-drug resistant P. yoelii in mice.
A series of new amino functionalized 1,2,4-trioxepanes 8-16 and ester functionalized 1,2,4-trioxepanes 17-19 have been synthesized and evaluated against multi-drug resistant Plasmodium yoelii in Swiss mice. Amino functionalized trioxepanes 14, the most active compound of the series, showed 100% clearance of parasitaemia by oral route on day 4 and 75% protection to the treated mice beyond day 28. Topics: Administration, Oral; Animals; Antimalarials; Artemisinins; Combinatorial Chemistry Techniques; Drug Resistance, Multiple; Heterocyclic Compounds; Mice; Parasitemia; Plasmodium yoelii; Propanols; Structure-Activity Relationship | 2008 |