TY - JOUR
T1 - Design, synthesis, inhibitory activity, and SAR studies of hydrophobic p-aminosalicylic acid derivatives as neuraminidase inhibitors
AU - Zhang, Jie
AU - Wang, Qiang
AU - Fang, Hao
AU - Xu, Wenfang
AU - Liu, Ailin
AU - Du, Guanhua
PY - 2008/4/1
Y1 - 2008/4/1
N2 - A series of hydrophobic p-aminosalicylic acid derivatives containing a lipophilic side chain at C-2 and an amino or guanidine at C-5 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 available p-aminosalicylic acid (PAS) using a suitable synthetic strategy. These compounds showed potent inhibitory activity against influenza A NA. Within this series, six compounds, 11, 12, 13e, 16e, 17c, and 18e, have the good potency (IC50 = 0.032-0.049 μM), which are compared to Oseltamivir (IC50 = 0.021 μM) and could be used as lead compounds in the future.
AB - A series of hydrophobic p-aminosalicylic acid derivatives containing a lipophilic side chain at C-2 and an amino or guanidine at C-5 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 available p-aminosalicylic acid (PAS) using a suitable synthetic strategy. These compounds showed potent inhibitory activity against influenza A NA. Within this series, six compounds, 11, 12, 13e, 16e, 17c, and 18e, have the good potency (IC50 = 0.032-0.049 μM), which are compared to Oseltamivir (IC50 = 0.021 μM) and could be used as lead compounds in the future.
KW - Influenza
KW - Neuraminidase inhibitor
KW - SAR study
KW - p-Aminosalicylic acid derivatives
UR - https://www.scopus.com/pages/publications/41649108175
U2 - 10.1016/j.bmc.2008.01.036
DO - 10.1016/j.bmc.2008.01.036
M3 - 文章
C2 - 18304821
AN - SCOPUS:41649108175
SN - 0968-0896
VL - 16
SP - 3839
EP - 3847
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 7
ER -