Design, synthesis, inhibitory activity, and SAR studies of hydrophobic p-aminosalicylic acid derivatives as neuraminidase inhibitors

J Zhang, Q Wang, H Fang, W Xu, A Liu, G Du

Index: Zhang, Jie; Wang, Qiang; Fang, Hao; Xu, Wenfang; Liu, Ailin; Du, Guanhua Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 7 p. 3839 - 3847

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Citation Number: 31

Abstract

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 ...