Pritelivir (BAY 57-1293) (BAY 57-1293) is a potent helicase-primase inhibitor with active against HSV-1 and HSV-2 (IC50: 20 nM).

HSV1/HSV2:20 nM, HSV2:20 nM

In models of lethal disseminated herpes infection in mice and rats, as well as in a mouse model simulating the spread of shingles-like skin disease, BAY57-1293 (administered orally at doses of 0.5/15 mg/kg) exhibited potent antiviral activity. This compound also showed similar efficacy in a mouse model of ocular herpes.

BAY57-1293 exhibits a dose-dependent direct inhibition of the viral helicase-primase complex's ATPase activity. It also demonstrates significant antiviral activity against acyclovir-resistant herpes simplex virus mutants. Additionally, in green monkey kidney cells, BAY57-1293 reduces the levels of Aβ and P-tau induced by herpes simplex virus type 1.

In vitro procaspase-3 activation: Procaspase-3 is expressed and purified in Escherichia coli. Various concentrations of PAC-1 are added to 90 μL of a 50 ng/mL of procaspase-3 in caspase assay buffer in a 96-well plate, The plate is incubated for 12 hours at 37 °C. A 10 μL volume of a 2 mM solution of caspase-3 peptidic substrate acetyl Asp-Glu-Val-Asp-p-nitroanilide (Ac-DEVD-pNa) in caspase assay buffer is then added to each well. The plate is read every 2 minutes at 405 nm for 2 hours in a Spectra Max Plus 384 well plate reader. The slope of the linear portion for each well is determined, and the relative increase in activation from untreated control wells is calculated.