九价烯酸合物作为强大的抑制剂,阻断流感A病毒的进入
Liang Shao1, Yangqing Su1, Yuan Zhang1
1Medical School of Kunming University of Science and Technology, Kunming, Yunnan, 650500, China.
European journal of medicinal chemistry
|June 24, 2023
概括
烯酸非氨基表现出强大的抗病毒活性对抗流感A和B病毒,通过向血凝蛋白. 这种新的多价值策略为开发新的流感病毒抑制剂提供了一个有希望的方法.
科学领域:
- 病毒学 病毒学
- 药用化学 医学化学
- 药物发现 药物发现 药物发现
背景情况:
- 流感大流行对全球健康构成重大威胁,病毒的高传染性和遗传变异性加剧了这一威胁.
- 开发有效的抗流感抗病毒药物仍然具有挑战性.
- 醇酸 (OA) 和其衍生物通过抑制流感与宿主细胞相互作用来证明其抗病毒功效.
研究的目的:
- 设计和合成使用多价值结构-活性结合策略的新型oleanolic 酸非amer.
- 为了评估这些合成化合物对流感病毒的体外抗病毒活性.
- 为了研究最强大的非氨基体的作用机制.
主要方法:
- 使用铜 (I) 催化酸循环添加 (CuAAC) 反应合成烯酸非氨基化合物.
- 在体外评估抗病毒活性对抗流感A (H1N1) 和流感B菌株.
- 确定半最大抑制度 (IC50) 的值.
- 机械研究以确定标蛋白 (血凝素).
主要成果:
- 化合物15是一种烯酸非胺基,对流感A/WSN/33 (H1N1) 具有强烈的抗病毒活性,IC50为5.23μM,与oseltamivir相当.
- 合成的nonamers也显示了抗病毒疗效对B型流感病毒.
- 机械学研究证实,这些烯酸非氨基有效向流感血质素 (HA) 蛋白.
结论:
- 多价值结构-活性结合策略对于设计强大的流感病毒抑制剂是有效的.
- 烯酸非氨基体代表了对抗流感A和B的有前途的抗病毒药物.
- 用多价值化合物向流感HA蛋白是一种可行的治疗方法.
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