摘要：Previous study on in vitro antiplasmodial activity of diaza phenanthrene analogs indicated that the 1,10-phenanthroline skeleton represents a potential antimalarial leader compound. Based on those skeletons, six derivatives of N -alkyl and N -benzyl-1,10-phenanthroline were synthesized and the in vitro antiplasmodial activities was evaluated. This paper reported the in vivo antiplasmodial activity study of the 1,10-phenanthroline derivatives performed by the classical 4-day suppressive test against Plasmodium berghei . Acute toxicity of each compound was determined after a single injection of the compound intraperitoneally in Swiss mice. The 50% effective dose (ED50) of the compound ranged from 2.08 to 50.93 mg/kg of body weight, and the therapeutic indices (TIs) ranged from 2.06 to 7.57 except (1)- N -benzyl-1,10-phenantrolinium iodide, which was 58.38. All of the 1,10-phenanthroline derivatives had in vivo antiplasmodial activity and (1)- N -benzyl-1,10-phenantrolinium iodide was the most potent.
关键词：1,10-phenanthroline;antiplasmodial;acute toxicity;therapeutic index
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