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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

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

Author(s): Jie Zhang, Wenfang Xu, Ailin Liu and Guanhua Du

Volume 4, Issue 3, 2008

Page: [206 - 209] Pages: 4

DOI: 10.2174/157340608784325151

Price: $65


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.

Keywords: Influenza virus, Neuraminidase, inhibitor, pyrrolidine derivatives

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