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2-(3,4-二氯苯氧基)-5-硝基苯甲腈(MDL-860)在体外对微小核糖核酸病毒的活性。

Activity of 2-(3,4-dichlorophenoxy)-5-nitrobenzonitrile (MDL-860) against picornaviruses in vitro.

作者信息

Powers R D, Gwaltney J M, Hayden F G

出版信息

Antimicrob Agents Chemother. 1982 Oct;22(4):639-42. doi: 10.1128/AAC.22.4.639.

Abstract

The newly synthesized compound 2-(3,4-dichlorophenoxy)-5-nitrobenzonitrile (MDL-860) has been found to inhibit picornavirus replication. In multiple growth cycle experiments, 1 microgram of MDL-860 per ml caused a reduction in virus yield of at least 1.0 log10 50% tissue culture infectious doses per 0.2 ml for 8 of 10 enteroviruses and 72 of 90 rhinovirus serotypes. This antiviral activity was dependent on both compound concentration and virus inoculum size. At concentrations that had no toxic effects on cell cultures, MDL-860 did not inhibit cytopathic effect or hemadsorption activity due to coronavirus 229-E, vesicular stomatitis virus, herpes simplex virus type 1, adenovirus, influenza virus A, or parainfluenza virus 1. Compound concentrations up to 25 micrograms/ml did not cause cytopathic effect in short-term cultures of rhesus monkey, WI-38, or HeLa cells; 10 micrograms/ml did not inhibit the replication of HeLa cells. The mechanism of action of MDL-860 has not been defined, although it was not directly virucidal and appeared to inhibit picornaviruses specifically at an early step in the virus-host cell interaction.

摘要

新合成的化合物2-(3,4-二氯苯氧基)-5-硝基苯甲腈(MDL-860)已被发现可抑制微小核糖核酸病毒复制。在多次生长周期实验中,每毫升1微克的MDL-860使10种肠道病毒中的8种以及90种鼻病毒血清型中的72种每0.2毫升的病毒产量降低至少1.0 log10 50%组织培养感染剂量。这种抗病毒活性取决于化合物浓度和病毒接种量。在对细胞培养物无毒性作用的浓度下,MDL-860不抑制229-E冠状病毒、水泡性口炎病毒、1型单纯疱疹病毒、腺病毒、甲型流感病毒或1型副流感病毒引起的细胞病变效应或血细胞吸附活性。高达25微克/毫升的化合物浓度在恒河猴、WI-38或HeLa细胞的短期培养中未引起细胞病变效应;10微克/毫升不抑制HeLa细胞的复制。MDL-860的作用机制尚未明确,尽管它并非直接杀病毒,且似乎在病毒-宿主细胞相互作用的早期阶段特异性抑制微小核糖核酸病毒。

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