synthesis and antimalarial activity of novel dihydro-artemisinin derivatives

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ID: 256000
2011
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Abstract
The Plasmodium falciparum cysteine protease falcipain-2, one of the most promising targets for antimalarial drug design, plays a key role in parasite survival as a major peptide hydrolase within the hemoglobin degradation pathway. In this work, a series of novel dihydroartemisinin derivatives based on (thio)semicarbazone scaffold were designed and synthesized as potential falcipain-2 inhibitors. The in vitro biological assay indicated that most of the target compounds showed excellent inhibition activity against P. falciparum falcipain-2, with IC50 values in the 0.29–10.63 μM range. Molecular docking studies were performed to investigate the binding affinities and interaction modes for the inhibitors. The preliminary SARs were summarized and could serve as a foundation for further investigation in the development of antimalarial drugs.
Reference Key
wang2011moleculessynthesis Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Jian Wang;Jin Huang;Chun Guo;Wei Luo;Yang Liu;Weiqiang Lu;Kunqiang Cui
Journal Journal of ethnopharmacology
Year 2011
DOI
10.3390/molecules16064527
URL
http://www.mdpi.com/1420-3049/16/6/4527/
Keywords
synthesis Molecular docking studies antibacterial activity oleanolic acid fluoroquinolone phenylpropanoid glycosides synthesisorganic chemistry 5-(4-hydroxybenzyl)-2-thioxoimidazolidin-4-one esters

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