酞丁安类似物抗单纯疱疹病毒活性的比较研究

酞丁安对HSV-1与HSV-2具有明显的抑制作用。修饰酞丁安结构,合成了14种酞丁安类似物,并对这些类似物的抗病毒活性与细胞毒性进行了研究。在14种酞丁安类似物中,有6种具有抗单纯疱疹病毒活性。但用非洲绿猴肾细胞进行空斑抑制测定,仅有一种酞丁安类似物V8540对HSV-2具有强烈的抑制作用,其抗HSV-2活性较酞丁安高10倍左右。酞丁安类似物抗HSV活性的次序为:V 8540>V 8512>V 8509>V 8502>V 8501>V 8519。其它酞丁安类似物抗单纯疱疹病毒活性很低或完全没有活性。用Vero细胞检测各种酞丁安类似物的细胞毒性,结果证明,V 8540的细胞毒性较酞丁安高。大量快速增殖的Vero细胞在V8540作用下停止了生长。

Comparative studies on antiviral activity of several TDA analogs against HSV-2

Fourteen TDA analogs were synthesized and their antiviral and cytotoxic activities examined. Among the 14 TDA analogs 6 were found to be effective against HSV-2. Of the 6 compounds V8540 was shown to be most potent inhibitor of HSV-2 in a plaque inhibition assay in Vero cells. It is approximately 10 times more active against HSV-2 than TDA. The following order of decreasing activity against HSV-2 in Vero cells was found: V8540>V8512>V8509>V8502>V8501>V8519. The Other compounds were less effective or inactive. The cytotoxic activity of the analogs was also determined using Vero cells. The results indicate that the toxic effects of V8540 were higher than those of TDA. A large number of rapidly proliferating Vero cells exposed to V8540 stopped growing.