TY - JOUR
T1 - Design, synthesis, inhibitory activity, and SAR studies of pyrrolidine derivatives as neuraminidase inhibitors
AU - Zhang, Jie
AU - Wang, Qiang
AU - Fang, Hao
AU - Xu, Wenfang
AU - Liu, Ailin
AU - Du, Guanhua
PY - 2007/4/1
Y1 - 2007/4/1
N2 - A series of pyrrolidine derivatives were synthesized and evaluated for their ability to inhibit neuraminidase (NA) of influenza A virus (H3N2). All compounds were synthesized in good yields starting from commercially 4-hydroxy-l-proline using a suitable synthetic strategy. These compounds showed potent inhibitory activity against influenza A neuraminidase. Within this series, five compounds, 6e, 9c, 9e, 9f, and 10e, have good potency (IC50 = 1.56-2.71 μM) which are compared to that the NA inhibitor Oseltamivir (IC50 = 1.06 μM), and could be used as lead compoundS in the future.
AB - A series of pyrrolidine derivatives were synthesized and evaluated for their ability to inhibit neuraminidase (NA) of influenza A virus (H3N2). All compounds were synthesized in good yields starting from commercially 4-hydroxy-l-proline using a suitable synthetic strategy. These compounds showed potent inhibitory activity against influenza A neuraminidase. Within this series, five compounds, 6e, 9c, 9e, 9f, and 10e, have good potency (IC50 = 1.56-2.71 μM) which are compared to that the NA inhibitor Oseltamivir (IC50 = 1.06 μM), and could be used as lead compoundS in the future.
KW - Neuraminidase inhibitor
KW - Peptidomimetics
KW - Pyrrolidine derivatives
KW - SAR study
UR - https://www.scopus.com/pages/publications/33847636143
U2 - 10.1016/j.bmc.2007.01.020
DO - 10.1016/j.bmc.2007.01.020
M3 - 文章
C2 - 17287121
AN - SCOPUS:33847636143
SN - 0968-0896
VL - 15
SP - 2749
EP - 2758
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 7
ER -