Key result
Compound 4a3 demonstrated broad in vitro antiviral activity against influenza A (EC50 9 and 18 μm for A/H1N1 and A/H3N2) and influenza B viruses (EC50 33 μm).
Dihydro-alkyloxy-benzyl-oxopyrimidine derivatives, particularly compound 4a3, demonstrate promising in vitro antiviral activity against influenza A and B viruses through a novel mechanism of action.
May support preclinical influenza antiviral development; leaves open in vivo efficacy and clinical translation.
A series of novel dihydro-alkyloxy-benzyl-oxopyrimidine derivatives were synthesized and evaluated for their activity against influenza virus in Madin-Darby canine kidney cells. Four dihydro-alkyloxy-benzyl-oxopyrimidine derivatives (4a1, 4a2, 4a3, and 4d1) showed potent activity against influenza virus. Among them, compound 4a3 was the most promising lead with broad activity against influenza A (antiviral EC(50) values of 9 and 18 μm for the A/H1N1 and A/H3N2 subtype, respectively) and influenza B viruses (EC(50) : 33 μm). The antiviral mechanism of action of these dihydro-alkyloxy-benzyl-oxopyrimidine derivatives must be quite different from that of the currently approved anti-influenza virus drugs that target the viral M2 or neuraminidase proteins. The dihydro-alkyloxy-benzyl-oxopyrimidine derivatives represent a new avenue for further optimization and development of novel anti-influenza virus agents.
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Yu et al. (2011) studied Influenza virus. Dihydro-alkyloxy-benzyl-oxopyrimidine derivatives (compound 4a3) was evaluated on Antiviral activity (EC50). Compound 4a3 demonstrated broad in vitro antiviral activity against influenza A (EC50 9 and 18 μm for A/H1N1 and A/H3N2) and influenza B viruses (EC50 33 μm).
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