Aromatic amino analogues of artemisinin: synthesis and in vivo antimalarial activity

作者：Sriram Dharmarajan^*; Devakaram Ruth Vandana; Dinakaran Murugesan; Yogeeswari Perumal

来源：Medicinal Chemistry Research, 2010, 19(6): 524-532.

DOI：10.1007/s00044-009-9209-5

• Antimalarial activity
• Artemisinin
• Plasmodium yoelii nigeriensis

Nine orally active novel artemisinin derivatives were prepared from artemisinin by four-step synthesis, and the compounds were evaluated in the rodent model using multidrug resistant Plasmodium yoelii nigeriensis. All of the compounds exhibited antimalarial activities with the ED(50) ranging from 5.41 mg/kg-12.4 mg/kg. Among them, artemisinin derivative bearing N-(4-hydroxy-3-((4-phenylpiperazin-1-yl)methyl)phenyl) moiety (5f) was found to be the most active compound and was found to be three times more potent than artemisinin (ED(50) 16.4 mg/kg).

• 出版日期2010-7