1304538-58-6Relevant articles and documents
Discovery of Dihydro-Alkyloxy-Benzyl-Oxopyrimidines as Promising Anti-Influenza Virus Agents
Yu, Mingyan,Liu, Ailin,Du, Guanhua,Naesens, Lieve,Vanderlinden, Evelien,De Clercq, Erik,Liu, Xinyong
experimental part, p. 596 - 602 (2012/04/10)
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 EC50 values of 9 and 18μm for the A/H1N1 and A/H3N2 subtype, respectively) and influenza B viruses (EC50: 33μm). 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. Dihydro-alkyloxy-benzyl-oxopyrimidine (DABO) derivatives were discoveried as new anti-influenza agents. Among them, compound 4a3 was the most promising with broad activity against influenza A (A/H1N1 and A/H3N2 subtype) and influenza B virus.
