The antiviral action of a new drug, 5-amino-2-(dimethylaminoethyl)-benzo-[de]-isoquinolin-1.3-dione has been studied against herpes simplex type 2 (HSV-2) and adenovirus type 5 (Ad-5) grown in Vero cells. The concentration of the drug which gives a 5 log10 reduction in virus titer was 4 micrograms/ml (maximum tolerated concentration) for HSV-2. The anti-HSV-2 activity of this compound was one log. more powerful than that of iododeoxyuridine (IDU). At this concentration the drug shows virucidal activity against HSV-2. No inhibition was found when the drug was tested against Ad-5. The inhibition of virus production has been studied depending upon the amount of drug or virus, and drug addition-time after infection. Reversibility of inhibition after drug removal, and drug resistance in the presence of the drug have also been determined.
Two benzo[de]isoquinoline-diones, namely 5-nitro-2-(2-dimethylaminoethyl)-benzo[de]isoquinoline-1,3-dione and 5-nitro-2-[2-(1-pyrrolidine)-ethyl]-benzo[de]isoquino-line-1,3-dione, caused inhibition of the viral replication, when assayed against herpes simplex and vaccinia viruses in chick embryo cell cultures. Influenza and Sindbis virus replication were unaffected by these chemicals. Virucidal effects were unobserved. The inhibitory activity is time-related. Ocular and dermal infections with vaccinia virus in rabbits were prevented or disease severity reduced whenever they were treated with either one of these two drugs.
Aus den 4‐Pyridyl‐methyl‐amiden (I) entstehen die N‐Oxide (II), die bei der Acetylierung mit Acetanhydrid zu den acylierten Ethylendiaminen (III) kondensiert werden.
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