Antiplasmodial Activity and Acute Toxicity of N-alkyl and N-benzyl-1,10-Phenanthroline Derivatives in Mouse Malaria Model

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概要

• 論文の詳細を見る

• 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 (ED_<50>) of the compound ranged from 2.08 to 50.93mg/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.

• 公益社団法人日本薬学会の論文
• 2006-12-01

著者

• Wijayanti Mahardika

  Department Of Parasitology Faculty Of Medicine Gadjah Mada University

• Tahir Iqmal

  Department Of Chemistry Faculty Of Mathemathics And Natural Sciences Gadjah Mada University

• Sholikhah Eti

  Department of Pharmacology and Toxicology Faculty of Medicine, Gadjah Mada University

• Hadanu Ruslin

  Department of Chemistry Faculty of Mathemathics and Natural Sciences, Gadjah Mada University

• Sholikhah Eti

  Department Of Pharmacology And Toxicology Faculty Of Medicine Gadjah Mada University

• Hadanu Ruslin

  Department Of Chemistry Faculty Of Mathemathics And Natural Sciences Gadjah Mada University

関連論文

• Antiplasmodial Activity and Acute Toxicity of N-alkyl and N-benzyl-1,10-Phenanthroline Derivatives in Mouse Malaria Model

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