title: Design, synthesis, and preliminary evaluation of new pyrrolidine derivatives as neuraminidase inhibitors.
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 (IC(50)=1.56 approximately 2.40microM) which is compared to the NA inhibitor oseltamivir (IC(50)=1.06microM), and could be used as lead compound in the future.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44, Wenhuaxi Road, 250012, Ji'nan, Shandong, P.R.China.
authors.forename: Jie
authors.initials: J
authors.lastname: Zhang
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
authors.forename: Ailin
authors.initials: A
authors.lastname: Liu
authors.forename: Guanhua
authors.initials: G
authors.lastname: Du
mesh_terms: D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry; D053122:Influenza A Virus, H3N2 Subtype / Q000201:enzymology; D008958:Models, Molecular; D009439:Neuraminidase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D000998:Antiviral Agents; D011759:Pyrrolidines; D009439:Neuraminidase