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Design, synthesis, and activity of 5-cyano-2-thiacetyl aromatic pyrimidinone as DENV NS5 RdRp inhibitors / 药学学报
Yao Xue Xue Bao ; (12): 3379-3388, 2023.
Article in Zh | WPRIM | ID: wpr-999072
Responsible library: WPRO
ABSTRACT
To screen novel anti-dengue virus (DENV) NS5 RdRp enzyme inhibitors, a series of 5-cyano-2-thiacetoaryl pyrimidinone compounds were designed and synthesized by molecular hybridization method with HCV NS5B RdRp inhibitor 3jc and ZIKV NS5 RdRp inhibitor 4w as lead compounds. The anti-DENV activity of these compounds was evaluated by MTT assay and plaque assay and five compounds showed anti-DENV activity. The most active compound 7a'k showed better anti-DENV activity than that of the positive control ribavirin (EC50 = 7.86 μmol·L-1 vs EC50 = 18.07 μmol·L-1), and the other four compounds showed almost the same anti-DENV activity as ribavirin. Finally, the prediction and simulation of the binding mode through molecular provided new ideas for the further development of this new DENV NS5 RdRp inhibitor.
Key words
Full text: 1 Index: WPRIM Language: Zh Journal: Yao Xue Xue Bao Year: 2023 Type: Article
Full text: 1 Index: WPRIM Language: Zh Journal: Yao Xue Xue Bao Year: 2023 Type: Article