ベンツイミタゾール誘導体の抗ウイルス性(第1報) : ハイドロオキシアルキールベンツイミダゾール誘導体の合成と抗ウイルス性

概要

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In order to study the antiviral activity of benzimidazole derivatives, 2-(hydroxymethyl)-, 2-(α-hydroxyethyl)-, 2-(α-hydroxypropyl)-, 2-(α-hydroxybenzyl)-, 2-(β-hydroxyethyl)-, and 2-(β-hydroxypropyl)-benzimidazole and their 5 (or 6)-methyl, -chloro, -nitro, and -methoxy derivatives were sythesised by refluxing o-phenylenediamine, or either one of its 4-methyl, 4-chloro, 4-nitro, and 4-methoxy analogs with glycolic, lactic, α-hydroxybutylic, β-hydroxybutylic, mandelic acid, or cyanoethanol in 4N hydrochloric acid. The antiviral activity of these compounds on polio virus and adenovirus replication was examined by tissue culture method. The cytophathic effect and multiplication of polio virus was inhibited by 2-(α-hydroxybenzyl) benzimidazole derivatives, 2-(α-hydroxyethyl)-5 (or 6)-methoxy-, 2-(α-hydroxypropyl)-5 (or 6)-methoxy-, 2-(β-hydroxyethyl)-5 (or 6)-methyl-, and 2-(β-hydroxypropyl)-5 (or 6)-chlorobenzimidazole. Cytophathic effect of adenovirus was clearly inhibited by 2-(α-hydroxypropyl)-5 (or 6)-methyl-, 2-(α-hydroxypropyl)-5 (or 6)-nitro-, and 2-(α-hydroxybenzyl)-5 (or 6)-methylbenzimidazole.
1968-06-25