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KMID : 0043320120350091525
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Archives of Pharmacal Research
2012 Volume.35 No. 9 p.1525 ~ p.1531
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Synthesis and biological activities of novel artemisinin derivatives as cysteine protease falcipain-2 inhibitors
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Liu Yang
Lu Wei Qiang
Cui Kun Qiang
Luo Wei
Wang Jian
Guo Chun
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Abstract
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A series of novel artemisinin derivatives were synthesized from artemisinin and different anilines. All compounds were obtained as β-isomers. The target compounds were evaluated for inhibition activity against Plasmodium falciparum falcipain-2 in vitro, and most of them exhibited potent inhibition in the low micromolar range and proved to be new types of falcipain-2 inhibitors.
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KEYWORD
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Falcipain-2 inhibitor, Artemisinin derivatives, (thio)Semicarbazone derivatives, Synthesis, Inhibition activity, Antimalarial
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