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Design, Synthesis, and Preliminary Evaluation of New Pyrrolidine Derivatives as Neuraminidase Inhibitors

[ Vol. 4 , Issue. 3 ]


Jie Zhang, Wenfang Xu, Ailin Liu and Guanhua Du   Pages 206 - 209 ( 4 )


A series of pyrrolidine derivatives were designed and synthesized in good yields starting from commercially available 4-hydroxy-L-proline using a suitable synthetic strategy. And their ability to inhibit neuraminidase was evaluated. These compounds showed potent inhibitory activity against influenza A (H3N2) neuraminidase. Within this series, four compounds, 6e, 9c, 9f and 10e, have the good potency (IC50=1.56∼2.40μM) which is compared to the NA inhibitor oseltamivir (IC50=1.06μM), and could be used as lead compound in the future.


Influenza virus, Neuraminidase, inhibitor, pyrrolidine derivatives


Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44, Wenhuaxi Road, 250012, Ji'nan, Shandong, P.R.China.

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