抗ウイルス化合物(第10報)2-置換5-Alkyl-6-Hydroxy-4-methylpyimidine類の合成と抗インフルエンザウイルス活性

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2-Mercapto-(I), 2-methylthio-(II), 2-hydrazino-(III), and 2-(3,5-dimethyl-1-pyrazolyl)-5-alkyl-6-hydroxypyrimidines (IV) were synthesized and their anti-influenza virus activity was examined. Among the tested compounds, inhibitory activity was observed only in the 5-propyl compound (IVb) (50% inhibitory concn. 4.7 μg/ml, index 4.8) and 5-hexyl compound (IVc) (339 μg/ml, 6.3). However, almost all the compounds exhibited a virucidal activity, and especially 5-octyl (Id) (50% virucidal concn. 90 μg/ml, index 8.8) and 5-hexyl (IIIc) (130 μg/ml, 7.7) compounds were considerably active. Compounds which showed toxic concentration of more than 125 μg/ml against HeLa cells were tested in infected mice. When intraperitoneally administered at a level of 100 mg/kg, 5-decyl (Ie), 5-methyl (IIa), and 5-propyl (IIb) compounds and amantadine hydrochloride respectively showed 71,62,62,and 55% inhibition of the virus multiplication in the lungs. However, Ie was inactive when administered orally.
社団法人日本薬学会の論文
1976-03-25