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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。
Phthalidin on HSV-1 and HSV-2 has a significant inhibitory effect. Modification of phthalidin structure, synthesis of 14 kinds of phthalidine analogues, and antiviral activity of these analogs and cytotoxicity were studied. Of the 14 phthalidine analogues, 6 have anti-herpes simplex virus activity. However, in the test of plaque inhibition with African green monkey kidney cells, only one of the derivatives of phthalidine V8540 had a strong inhibitory effect on HSV-2, and its anti-HSV-2 activity was about 10 times higher than that of titradine. The order of the anti-HSV activity of the phthalidine analog was: V 8540> V 8512> V 8509> V 8502> V 8501> V 8519. Other phthalidin analogs have low or no activity against herpes simplex virus. The cytotoxicity of various phthalodine analogues was examined with Vero cells and the results demonstrated that V 8540 is more cytotoxic than docetudan. A large number of rapidly proliferating Vero cells stopped growing under the action of V8540.