抗 Virus 化合物 (第15報) : 5,6-Diphenyl-1,2,4-triazine-3-thiol とアルコール類との反応及び抗 Virus 活性

概要

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When 5,6-diphenyl-1,2,4-triazine-3-thiol was heated in methanol or ethanol under neutral conditions, the addition of methanol or ethanol across the N_4-C_5 bond occurred to give the corresponding 5-alkoxy-4,5-dihydro-5,6-diphenyl-1,2,4-triazine-3-thiol. Such reaction was not observed in 1-butanol. When the triazine derivative refluxed in 2-propanol, bis(5,6-diphenyl-1,2,4-triazin-3-yl) disulfide was obtained instead of the expected addition compound. Structurally similar compounds, 3-methylthio-5,6-diphenyl-1,2,4-triazine and 6-methyl-5-phenyl-1,2,4-triazine-3-thiol did not undergo such reaction. The synthesized compounds were examined mainly for activities against influenza viruses. 3-Mercapto- and 5-alkoxy-4,5-dihydro-3-mercapto-5,6-diphenyl-1,2,4-triazines exhibited 50% inhibitory concentrations of 12.5-63.1 μg/ml (Index 12.6-63.5) against influenza viruses such as A_0/PR-8,A_1/FM-1,A_1/Fukuoka, A_2/Adachi, A_2/Aichi, B/Lee, B/Kagoshima and Horse/Miami in the chorio-allantoic membrane culture.
社団法人日本薬学会の論文
1986-01-25