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N-苯基-N'-芳基或烷基硫脲衍生物对小鼠柯萨奇病毒感染的抗病毒活性。

Antiviral activity of N-phenyl-N'-aryl- or alkylthiourea derivatives in Coxsackie virus infections in mice.

作者信息

Galabov A S, Velichkova E H

出版信息

Antimicrob Agents Chemother. 1974 Jan;5(1):1-8. doi: 10.1128/AAC.5.1.1.

Abstract

The effect of five derivatives of N-phenyl-N'-aryl- or alkylthiourea-inhibitors of the multiplication of Coxsackie virus B1 and other picornaviruses in vitro-was tested in experimental infections with Coxsackie viruses B1, B3, A6, and A7 in newborn mice. Under the action of N-phenyl-N'-3-hydroxyphenylthiourea (no. 23) and N-phenyl-N'-4-carboxy-5-hydroxyphenylthiourea (no. 20) a two- to threefold reduction in mortality was observed, as well as an appreciable delay in the course of the disease (mean effective dose, lengthening by 2 to 6 days) after infection with Coxsackie viruses B1, B3, and A7. The infection with Coxsackie virus A6 was affected only by compound no. 23 and, at that, to a low degree. If the antiviral effect is to be obtained, the compounds must be applied daily (once subcutaneously) from the 24th to the 144th h after virus inoculation, a period which corresponds to the incubation period and the beginning of the manifested infection. On the basis of these data, as well as of the relatively high selectivity (therapeutic index of 3 to 20), the two indicated substances may be considered to be reliable antiviral chemotherapeutic agents.

摘要

在新生小鼠感染柯萨奇病毒B1、B3、A6和A7的实验中,测试了N-苯基-N'-芳基或烷基硫脲的五种衍生物(体外对柯萨奇病毒B1及其他小RNA病毒增殖的抑制剂)的作用。在N-苯基-N'-3-羟基苯基硫脲(第23号)和N-苯基-N'-4-羧基-5-羟基苯基硫脲(第20号)的作用下,观察到死亡率降低了两到三倍,并且在用柯萨奇病毒B1、B3和A7感染后,疾病进程出现明显延迟(平均有效剂量,延长2至6天)。柯萨奇病毒A6的感染仅受到第23号化合物的影响,而且程度较低。若要获得抗病毒效果,必须在病毒接种后第24小时至第144小时每天(皮下注射一次)应用这些化合物,这段时间对应潜伏期和显性感染的开始阶段。基于这些数据以及相对较高的选择性(治疗指数为3至20),上述两种物质可被视为可靠的抗病毒化疗药物。

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