Background:
Substituted pyrimidine derivatives (non-nucleoside) are found to be associated
with various biological activities. The various substituted pyrimidines are also having significant in vitro
activity against different DNA and RNA viruses. The present study focuses on the anti-PV activity of
new pyrimidines and their condensed derivatives.
Methods:
A series of novel pyrimidines and their condensed derivatives were synthesized and their
structures were confirmed by spectral data. Their antiviral activities against poliovirus type 3 (PV-3)
were evaluated in vitro. In cell culture, morphological changes observed in cells infected with polioviruses,
including cell rounding and detachment from the substrate, are generally termed cytopathic
effects (CPE). The effects of synthetic pyrimidines on PV amplification in a culture of the heteroploid
cell line, Vero 76 (African green monkey kidney cells) were investigated.
Results:
Bioassays in vitro showed that one of seven synthesized compounds, 7-(Benzenesulfonyl)-5-
benzyl-N-(prop-2-en-1-yl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine, has potent antiviral activity against
PV-3 (EC50 = 0.75 μM). The selectivity index of this compound is similar to that of pirodavir.
Conclusion:
The need for antiviral agents to treat PV-associated diseases remains great, but few options
currently exist. Here we show that substituted pyrimidine derivatives are a promising structure class of
chemical compounds for the development of antiviral drugs against PV infections.