Key result
Derivatives 3c and 3d demonstrate ~70% inhibition against vaccinia virus with modest HSV-1 activity.
Why the study?
New pyrazolo[4,3-c]quinolin-3-one ribonucleosides and their heterocycle moieties were synthesized to evaluate their antiviral activities against vaccinia virus and herpes simplex virus type 1.
Newly synthesized pyrazolo[4,3-c]quinolin-3-one derivatives demonstrate only modest antiviral activity against vaccinia virus and HSV-1.
Modest activity offers no clinical utility now; leaves open whether further optimization can yield viable antiviral candidates.
Several new pyrazolo[4,3-c]quinolin-3-one ribonucleosides (5a-g) and their corresponding heterocycle moieties (3a-g) were synthesized and evaluated against vaccinia virus (VV) and herpes simplex virus type 1 (HSV-1). The derivatives 3c and 3d showed modest inhibitory activity against vaccinia virus reaching 70% at a concentration of 100 microM. All heterocyclic compounds (3a-f) showed a modest inhibition against HSV-1, reaching the maximal inhibitory effect around 20-30%. The antiviral effects of most of the pyrazolo[4,3-c]quinolin-3-one ribonucleosides (5a-f) on VV and HSV were not impressive.
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Oliveira et al. (2004) studied Vaccinia virus (VV) and herpes simplex virus type 1 (HSV-1). Pyrazolo[4,3-c]quinolin-3-one ribonucleosides and heterocycle moieties was evaluated on Inhibitory activity against vaccinia virus and HSV-1. Derivatives 3c and 3d showed modest inhibitory activity against vaccinia virus (70% at 100 microM), while heterocyclic compounds showed 20-30% maximal inhibition against HSV-1.
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