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Novel Bis- and Tris-1,2,4-trioxanes: Synthesis and Antimalarial Activity against Multidrug-Resistant Plasmodium yoelii in Swiss Mice.

  作者 Singh, Chandan;Verma, Ved Prakash;Naikade, Niraj Krishna;Singh, Ajit Shankar;Hassam, Mohammad;Puri, Sunil K.;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-23;  页码  7581-7592  
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[摘要]A new series of bis-1,2,4-trioxanes and tris-1,2,4-trioxanes were prepd. and evaluated against multidrug-resistant Plasmodium yoelii in Swiss mice by oral route. Five cyclopentane-based bis-trioxanes and three cyclohexane-based bis-trioxanes showed promising activity. All of the tris-1,2,4-trioxanes were found to be inactive. Bis-trioxane I, the most active compd. of the series, provided 100% and 80% protection to infected mice at 48 and 24 mg/kg ?4 days, resp. The clin. useful drug b-arteether provided 100% and 20% protection at similar doses.

 
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