Baccichetti F, Carlassare F, Bordin F, Marciani Magno S, Gia O, Peron M
Farmaco Sci. 1980 Jun;35(6):481-9.
The activity of four tilorone analogous compounds against three different strains of E. coli bacteriophages T1, T2 and phiX-174, was studied. Among the compounds we tested, only a fluorene derivative (2,7-bis-2-[2-(diethylamino)acetyl]fluorene) yielded a high inhibition of phage growth, to a greater extent with respect to tilorone, used as a reference compound. This activity, not due to a toxic effect on the host bacteria, did not appear connected with a complex formation between the drug and DNA. In fact, among the studied compounds, this is not the one showing the highest binding parameters with DNA; in addition, when the mature virions were incubated in the presence of the drug and then diluted and assayed for their plaque-forming capacity, this drug turned out to be practically ineffective. Fluorene derivative appears to be an antiviral drug acting on an unidentified metabolic process of phage growth, and therefore it is a model for new antiviral drugs showing a selective activity.
研究了四种替洛隆类似化合物对三种不同菌株的大肠杆菌噬菌体T1、T2和phiX - 174的活性。在我们测试的化合物中,只有一种芴衍生物(2,7 - 双 - 2 - [2 - (二乙氨基)乙酰基]芴)对噬菌体生长产生了高度抑制,相对于用作参考化合物的替洛隆,抑制程度更大。这种活性并非由于对宿主细菌的毒性作用,似乎也与药物和DNA之间的复合物形成无关。事实上,在所研究的化合物中,它并不是与DNA结合参数最高的;此外,当成熟病毒粒子在药物存在下孵育,然后稀释并检测其形成噬菌斑的能力时,这种药物实际上是无效的。芴衍生物似乎是一种作用于噬菌体生长未明代谢过程的抗病毒药物,因此它是显示选择性活性的新型抗病毒药物的一个模型。