The activity of dispiro peroxides against Fasciola hepatica

Dispiro 1,2,4-trioxanes and 1,2,4,5-tetraoxanes had superior efficacy against Fasciola hepatica than the corresponding ozonides (1,2,4-trioxolanes). For highest efficacy, spiroadamantane and carboxymethyl substructures were required. Three compounds completely cured F. hepatica-infected mice at sing...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-09, Vol.21 (18), p.5320-5323
Hauptverfasser:	Wang, Xiaofang, Zhao, Qingjie, Vargas, Mireille, Dong, Yuxiang, Sriraghavan, Kamaraj, Keiser, Jennifer, Vennerstrom, Jonathan L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Artemisinin Biological and medical sciences chemistry Dose-Response Relationship, Drug Fasciola hepatica Fasciola hepatica - drug effects Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacology Medical sciences Mice Molecular Structure Peroxide peroxides Pharmacology. Drug treatments Spiro Compounds - chemical synthesis Spiro Compounds - chemistry Spiro Compounds - pharmacology Stereoisomerism Tetraoxanes - chemical synthesis Tetraoxanes - chemistry Tetraoxanes - pharmacology
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Zusammenfassung:	Dispiro 1,2,4-trioxanes and 1,2,4,5-tetraoxanes had superior efficacy against Fasciola hepatica than the corresponding ozonides (1,2,4-trioxolanes). For highest efficacy, spiroadamantane and carboxymethyl substructures were required. Three compounds completely cured F. hepatica-infected mice at single oral doses of 50mg/kg and two were partially curative at single doses of 25mg/kg.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.07.024