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New functionalized 1,2,4-trioxepanes: synthesis and antimalarial activity against multi-drug resistant P. yoelii in
Chandan Singh1, Shilpi Pandey, Ambuj K Kushwaha
1Division of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow 226001, India. chandancdri@yahoo.com
Bioorganic & Medicinal Chemistry Letters
|September 16, 2008
Abstract:
A series of new amino functionalized 1,2,4-trioxepanes 8-16 and ester functionalized 1,2,4-trioxepanes 17-19 have been synthesized and evaluated against multi-drug resistant Plasmodium yoelii in Swiss mice. Amino functionalized trioxepanes 14, the most active compound of the series, showed 100% clearance of parasitaemia by oral route on day 4 and 75% protection to the treated mice beyond day 28.
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