title: Simple analogues of qinghaosu (artemisinin).
abstract: A series of 1,2,4-trioxanes were synthesized in which the key peroxy bonds were installed through a molybdenum-catalyzed perhydrolysis of the epoxy rings. A core structure was identified that may serve as a promising lead structure for further investigations because of its high antimalarial activity (comparable to that of artesunate and chloroquine), apparent potential for scale-up and derivatization, and facile monitoring/tracing by using UV light.
authors.affiliation: State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institution of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai 200032, China.
authors.forename: Yun
authors.initials: Y
authors.lastname: Li
authors.forename: Hong-Dong
authors.initials: HD
authors.lastname: Hao
authors.forename: Sergio
authors.initials: S
authors.lastname: Wittlin
authors.forename: Yikang
authors.initials: Y
authors.lastname: Wu
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry*; D037621:Artemisinins / Q000138:chemical synthesis / Q000737:chemistry*; D002384:Catalysis; D003500:Cyclization; D004852:Epoxy Compounds / Q000737:chemistry; D006571:Heterocyclic Compounds / Q000737:chemistry; D008982:Molybdenum / Q000737:chemistry; D013329:Structure-Activity Relationship; D014466:Ultraviolet Rays
chemical_list: C503429:1,2,4-trioxane; D000962:Antimalarials; D037621:Artemisinins; D004852:Epoxy Compounds; D006571:Heterocyclic Compounds; D008982:Molybdenum; C031327:artemisinin