Dubovi E J, Geratz J D, Shaver S R, Tidwell R R
Antimicrob Agents Chemother. 1981 Apr;19(4):649-56. doi: 10.1128/AAC.19.4.649.
Several aromatic mono- and diamidines were found to block cell fusion induced by respiratory syncytial virus. The best inhibitors were able to achieve complete suppression of syncytium formation at a concentration of 1.0 microM. Inhibition occurred in respiratory syncytial virus-infected HEp-2 and CV-1 cells, but the same inhibitors were ineffective in preventing fusion induced by parainfluenza virus type 3. The fusion inhibitors did not reduce single-cycle virus yields, but did reduce multiple-cycle yields. In addition, the active compounds caused a significant retardation of respiratory syncytial virus penetration. The mechanism by which amidines interfere with respiratory syncytial virus-host cell interactions is unknown, but parallels can be drawn between antiviral activity and the ability of the compounds to inhibit certain trypsin-like proteases.
发现几种芳香族单脒和双脒可阻断呼吸道合胞病毒诱导的细胞融合。最佳抑制剂能够在浓度为1.0微摩尔时完全抑制多核巨细胞的形成。在呼吸道合胞病毒感染的HEp-2和CV-1细胞中发生了抑制作用,但相同的抑制剂在预防3型副流感病毒诱导的融合方面无效。融合抑制剂不会降低单周期病毒产量,但会降低多周期产量。此外,活性化合物会显著延缓呼吸道合胞病毒的穿透。脒干扰呼吸道合胞病毒-宿主细胞相互作用的机制尚不清楚,但可以在抗病毒活性与化合物抑制某些类胰蛋白酶的能力之间找到相似之处。