新型抗鼻病毒化合物R 61837的体外活性
In vitro activity of R 61837, a new antirhinovirus compound.
作者信息
Andries K, Dewindt B, De Brabander M, Stokbroekx R, Janssen P A
机构信息
Janssen Research Foundation, Beerse, Belgium.
出版信息
Arch Virol. 1988;101(3-4):155-67. doi: 10.1007/BF01310997.
Abstract
R 61837 or 3-methoxy-6-[4-(3-methylphenyl)-1-piperazinyl]pyridazine is a new and potent inhibitor of rhinoviruses at concentrations not inhibitory to HeLa cell growth. Different rhinovirus serotypes varied widely in their susceptibility to the antiviral agent. The MICs for 50% CPE reduction ranged from 0.004 to 15 micrograms/ml. The yields of the most susceptible serotypes were reduced by a factor of 1,000 to 10,000 after single round high multiplicity infections in presence of low concentrations of the compound. The inactivation of some but not all serotypes in a time-, concentration- and temperature-dependent way by R 61837 indicated a direct interaction between the drug and the viral particles. The antiviral activity of the compound was confirmed in the human target cells for rhinoviruses by experiments using nasal polyp explant cultures.
摘要
R 61837或3-甲氧基-6-[4-(3-甲基苯基)-1-哌嗪基]哒嗪是一种新型强效鼻病毒抑制剂，其浓度对HeLa细胞生长无抑制作用。不同的鼻病毒血清型对该抗病毒药物的敏感性差异很大。使50%细胞病变效应减少的最低抑菌浓度范围为0.004至15微克/毫升。在低浓度化合物存在下进行单轮高复数感染后，最敏感血清型的产量降低了1000至10000倍。R 61837以时间、浓度和温度依赖的方式使部分而非全部血清型失活，表明该药物与病毒颗粒之间存在直接相互作用。通过使用鼻息肉外植体培养物的实验，在人鼻病毒靶细胞中证实了该化合物的抗病毒活性。
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