Archives of Pharmacal Research

, Volume 35, Issue 9, pp 1525–1531

Synthesis and biological activities of novel artemisinin derivatives as cysteine protease falcipain-2 inhibitors

  • Yang Liu
  • Wei-Qiang Lu
  • Kun-Qiang Cui
  • Wei Luo
  • Jian Wang
  • Chun Guo
Research Article Drug Design and Discovery

DOI: 10.1007/s12272-012-0902-4

Cite this article as:
Liu, Y., Lu, WQ., Cui, KQ. et al. Arch. Pharm. Res. (2012) 35: 1525. doi:10.1007/s12272-012-0902-4

Abstract

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.

Key words

Falcipain-2 inhibitor Artemisinin derivatives (thio)Semicarbazone derivatives Synthesis Inhibition activity Antimalarial 

Copyright information

© The Pharmaceutical Society of Korea and Springer Science+Business Media Dordrecht 2012

Authors and Affiliations

  • Yang Liu
    • 1
  • Wei-Qiang Lu
    • 2
  • Kun-Qiang Cui
    • 2
  • Wei Luo
    • 1
  • Jian Wang
    • 1
  • Chun Guo
    • 1
  1. 1.Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical EngineeringShenyang Pharmaceutical UniversityShenyangChina
  2. 2.School of PharmacyEast China University of Science and TechnologyShanghaiChina

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