N-Long-chain Monoacylated Derivatives of 2,6-Diaminopyridine with Antiviral Activity

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概要

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• N-Monoacyl-2,6-diaminopyridines (2a-c) and N,N'-diacyl-2,6-diaminopyridines (3a-c) were synthesized from 2,6-diaminopyridine by acylation with the corresponding acyl halide or by dehydration with the corresponding carboxylic acid using 1,3-dicyclohexylcarbodiimide (DCC). The antiviral activities of N-monoacyl- and N,N'-diacyl-2,6-diaminopyridines (2a-c and 3a-c) were estimated using plaque reduction assay with HSV-1. All N-monoacyl derivatives (2a-c) showed significant anti-herpes simplex virus (HSV)-1 activity (EC_<50>=15.3-18.5μg/ml). The CC_<50> values of 2a-c measured using Vero cells ranged at 37.5-50.0μg/ml. These compounds showed no significant antibacterial activities with Escherichia coli or Staphylococcus aureus even at a concentration of 1mg/ml. The N,N'-diacyl derivatives (3a-c) showed no significant anti-HSV-1 activity.

• 公益社団法人日本薬学会の論文
• 2007-01-01

著者

• Mibu N

  Faculty Of Pharmaceutical Sciences Fukuoka University

• YOKOMIZO Kazumi

  Faculty of Medical and Pharmaceutical Sciences, Kumamoto University

• Uyeda Masaru

  Dep. Of Nutrition Sci. Facultiy Of Living Sci. Shokei Univ.

• Uyeda Masaru

  Laboratory Of Pharmaceutical Microbiology Faculty Of Medical And Pharmaceutical Sciences Kumamoto Un

• Uyeda Masaru

  Shokei University

• Yokomizo K

  Kumamoto Univ. Kumamoto Jpn

• Udayama M

  Kumamoto Univ. Kumamoto Jpn

• Miyata Takeshi

  Faculty Of Pharmaceutical Sciences Sojo University

• Mibu Nobuko

  Faculty Of Pharmaceutical Sciences Fukuoka University

• Yokomizo Kazumi

  Laboratory Of Pharmaceutical Microbiology Faculty Of Medical And Pharmaceutical Sciences Kumamoto Un

• Yokomizo Kazumi

  Faculty Of Pharmaceutical Sciences Kumamoto University

• KASHIGE Nobuhiro

  Faculty of Pharmaceutical Sciences, Fukuoka University

• MIAKE Fumio

  Faculty of Pharmaceutical Sciences, Fukuoka University

• SUMOTO Kunihiro

  Faculty of Pharmaceutical Sciences, Fukuoka University

• Udayama Manabu

  Faculty Of Pharmaceutical Sciences Kumamoto University

• Uyeda Masaru

  Department Of Pharmaceutical Microbiology Faculty Of Medical And Pharmaceutical Sciences Kumamoto Un

• Miake F

  Faculty Of Pharmaceutical Sciences Fukuoka University

• Miake Fumio

  Faculty Of Pharmaceutical Sciences Fukuoka University

• Sumoto K

  Faculty Of Pharmaceutical Sciences Fukuoka University

• Sumoto Kunihiro

  Fukuoka Univ. Fukuoka Jpn

• Sumoto Kunihiro

  Faculty Of Pharmaceutical Sciences Fukuoka University

• Kashige Nobuhiro

  Faculty Of Pharmaceutical Sciences Fukuoka University

• Sumoto Kunihiro

  Faculty of Pharmaceutical Science, Fukuoka University

• Miake Fumio

  Faculty of Pharmaceutical Science, Fukuoka University

• Kashige Nobuhiro

  Faculty of Pharmaceutical Science, Fukuoka University

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