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

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

Volume: 4 Issue: 3

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

Affiliation:

Keywords: Influenza virus, Neuraminidase, inhibitor, pyrrolidine derivatives

Abstract: 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.

Cite this article as:

Zhang Jie, Xu Wenfang, Liu Ailin and Du Guanhua, Design, Synthesis, and Preliminary Evaluation of New Pyrrolidine Derivatives as Neuraminidase Inhibitors, Medicinal Chemistry 2008; 4 (3) . https://dx.doi.org/10.2174/157340608784325151