COMPARATIVE STUDIES ON ANTIVIRAL ACTIVITY OF SEVERAL TDA ANALOGS AGAINST HSV-2^Δ

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.