Abstract |
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) = 15.3-18.5 microg/ml). The CC(50) values of 2a-c measured using Vero cells ranged at 37.5-50.0 microg/ml. These compounds showed no significant antibacterial activities with Escherichia coli or Staphylococcus aureus even at a concentration of 1 mg/ml. The N,N'-diacyl derivatives (3a-c) showed no significant anti-HSV-1 activity.
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Authors | Nobuko Mibu, Kazumi Yokomizo, Nobuhiro Kashige, Fumio Miake, Takeshi Miyata, Masaru Uyeda, Kunihiro Sumoto |
Journal | Chemical & pharmaceutical bulletin
(Chem Pharm Bull (Tokyo))
Vol. 55
Issue 1
Pg. 111-4
(Jan 2007)
ISSN: 0009-2363 [Print] Japan |
PMID | 17202712
(Publication Type: Journal Article)
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Chemical References |
- Antiviral Agents
- Pyridines
- 2,6-diaminopyridine
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Topics |
- Acylation
- Animals
- Antiviral Agents
(chemistry, pharmacology)
- Cell Line
- Chlorocebus aethiops
- Microbial Sensitivity Tests
- Pyridines
(chemistry, pharmacology)
- Vero Cells
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