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Discovery of Dihydro‐Alkyloxy‐Benzyl‐Oxopyrimidines as Promising Anti‐Influenza Virus Agents

Year: 2011
Type: article
Abstract: 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.
DOI: 10.1111/j.1747-0285.2011.01180.x
Authors: Mingyan Yu, Ailin Liu, Guanhua Du, Lieve Naesens, Evelien Vanderlinden, Erik De Clercq, Xinyong Liu
Language: English
Subfield: Epidemiology
Field: Medicine
Open Access status: green
Funders: Shandong University, National Natural Science Foundation of China, Fonds Wetenschappelijk Onderzoek, Vlaamse regering, Independent Innovation Foundation of Shandong University, Specialized Research Fund for the Doctoral Program of Higher Education of China
OpenAlex ID: W1834216596
FWCI: 0.652
Cites: 16
Cited by: 8
Related to: 10