Bioorganic & Medicinal Chemistry Letters 2012-02-15

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

Koneni V Sashidhara, Abdhesh Kumar, K Bhaskara Rao, Vikas Kushwaha, Kirti Saxena, P K Murthy

文献索引：Bioorg. Med. Chem. Lett. 22 , 1527-32, (2012)

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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.Copyright © 2012 Elsevier Ltd. All rights reserved.