TY - JOUR
T1 - The activity of dispiro peroxides against Fasciola hepatica
AU - Wang, Xiaofang
AU - Zhao, Qingjie
AU - Vargas, Mireille
AU - Dong, Yuxiang
AU - Sriraghavan, Kamaraj
AU - Keiser, Jennifer
AU - Vennerstrom, Jonathan L.
N1 - Funding Information:
This investigation received financial support from NIH ( R21AI076783 ) and the Swiss National Science Foundation (Project No. PPOOA-114941 ).
PY - 2011/9/15
Y1 - 2011/9/15
N2 - 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 50 mg/kg and two were partially curative at single doses of 25 mg/kg.
AB - 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 50 mg/kg and two were partially curative at single doses of 25 mg/kg.
KW - Artemisinin
KW - Fasciola hepatica
KW - Peroxide
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U2 - 10.1016/j.bmcl.2011.07.024
DO - 10.1016/j.bmcl.2011.07.024
M3 - Article
C2 - 21802291
AN - SCOPUS:80051931320
SN - 0960-894X
VL - 21
SP - 5320
EP - 5323
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 18
ER -