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In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: A new class of antifilarial agents

  作者 Sashidhara, KV; Kumar, A; Rao, KB; Kushwaha, V; Saxena, K; Murthy, PK  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2012年22-4;  页码  1527-1532  
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[摘要]A series of 3,6-epoxy [1,5] dioxocines were synthesized and evaluated for their antifilarial activity against adult parasites of human lymphatic filarial parasite Brugia malayi (sub-periodic strain) in vitro. Out of these, six compounds (4a-f) possessed improved in vitro anti-filarial activity and examples 4d and 4f were also found to be active in the in vivo experiments. These results demonstrate that 3,6-epoxy [1,5] dioxocines exhibits potent antifilarial activity and might be developed into a new class of antifilarial drug. (C) 2012 Elsevier Ltd. All rights reserved.

 
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