3-(Substituted benzenesulfonylamino)-5,6-di(p-substituted phenyl)-1,2,4-triazine 類の抗 Virus 及び抗菌活性

概要

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3-(Substituted benzenesulfonylamino)-5,6-di(p-substituted phenyl)-1,2,4-triazines were synthesized and examined for their antimicrobial activities against influenza virus A_2/Adachi strain and micro-organisms parasitic to animals and plants. 3-(Benzenesulfonylamino)-5,6-di(p-chloro- and p-bromo-phenyl), 3-(4-fluorobenzenesulfonylamino)-5,6-di(p-fluorophenyl), 3-(2,5-dichlorobenzenesulfonylamino)-5,6-di(p-butoxyphenyl), 3-(3-nitrobenzenesulfonylamino)-5,6-di(p-chlorophenyl) and 3-(3-aminobenzenesulfonylamino)-5,6-di(p-butoxyphenyl)-1,2,4-triazines were highly active against the influenza virus. Their 50% inhibitory concentrations were 4.4-19.8 μg/ml and 50% virucidal concentrations were 4.4-10 μg/ml. p-Substitution of halo group or alkoxy group having suitable chain length on 5- and 6-phenyl rings of 1,2,4-triazine enhanced especially the virucidal activity. Satisfactory quantitative structure-activity relationships were obtained for the inhibitory activity against the virus and for toxicity to chorio-allantoic membrane. About half of these compounds showed minimum inhibitory concentrations of 50-100 μg/ml against Mycoplasma gallisepticum and <6.3-100 μg/ml against Erwinia aroideae and Corynebacterium michiganense.
社団法人日本薬学会の論文
1988-01-25