吡咯烷苯并酸类流感病毒神经氨酸酶抑制剂：疏水性侧链影响 A 型亚型选择性。
Pyrrolidinobenzoic acid inhibitors of influenza virus neuraminidase: the hydrophobic side chain influences type A subtype selectivity.
机构信息
Department of Chemistry, University of Alabama at Birmingham, Birmingham, AL 35294, USA.
出版信息
Bioorg Med Chem. 2012 Jul 15;20(14):4582-9. doi: 10.1016/j.bmc.2012.05.001. Epub 2012 May 17.
Neuraminidase (NA) plays a critical role in the life cycle of influenza virus and is a target for new therapeutic agents. A series of influenza neuraminidase inhibitors with the pyrrolidinobenzoic acid scaffold containing lipophilic side chains at the C3 position have been synthesized and evaluated for influenza neuraminidase inhibitory activity. The size and geometry of the C3 side chains have been modified in order to investigate structure-activity relationships. The results indicated that size and geometry of the C3-side chain are important for selectivity of inhibition against N1 versus N2 NA, important type A influenza variants that infect man, including the highly lethal avian influenza.
神经氨酸酶（NA）在流感病毒的生命周期中起着关键作用，是新治疗药物的靶标。已经合成了一系列含有亲脂性侧链的吡咯烷苯甲酸骨架的流感神经氨酸酶抑制剂，并对其流感神经氨酸酶抑制活性进行了评估。为了研究构效关系，对 C3 位侧链的大小和几何形状进行了修饰。结果表明，C3-侧链的大小和几何形状对 N1 与 N2 NA 抑制的选择性很重要，N1 和 N2 NA 是感染人类的重要 A 型流感病毒，包括高致死性禽流感。
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