Design, synthesis, inhibitory activity, and SAR studies of hydrophobic p-aminosalicylic acid derivatives as neuraminidase inhibitors
Design, synthesis, inhibitory activity, and SAR studies of hydrophobic p-aminosalicylic acid derivatives as neuraminidase inhibitors
复制标题
疏水性对氨基水杨酸衍生物神经氨酸酶抑制剂的设计、合成、抑制活性和 SAR 研究
DOI：
10.1016/j.bmc.2008.01.036
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发表时间：
2008-04-01
影响因子：
3.5
通讯作者：
Du, Guanhua
中科院分区：
文献类型：
--
作者：
Zhang, Jie;Wang, Qiang;Du, Guanhua
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 mu M), which are compared to Oseltamivir (IC50 = 0.021 mu M) and could be used as lead compounds in the future. (C) 2008 Elsevier Ltd. All rights reserved.
