Submit Manuscript  

Article Details


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

[ Vol. 4 , Issue. 3 ]

Author(s):

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

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.

Keywords:

Influenza virus, Neuraminidase, inhibitor, pyrrolidine derivatives

Affiliation:

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



Read Full-Text article