新型 2,4-二取代喹唑啉衍生物的设计、合成及抗流感 A 病毒活性研究。
Design, synthesis and anti-influenza A virus activity of novel 2,4-disubstituted quinazoline derivatives.
机构信息
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.
出版信息
Bioorg Med Chem Lett. 2020 Jun 1;30(11):127143. doi: 10.1016/j.bmcl.2020.127143. Epub 2020 Mar 27.
Four 2,4-disubstituted quinazoline series containing various amide moieties were designed and synthesized as new anti-influenza A virus agents using the strategies of bio-isosterism and scaffold hopping. Many of them exhibit potent in vitro anti-influenza A virus activity and low cytotoxicity (CC: >100 μM). Particularly, compounds 10a5 and 17a show better activity (IC: 3.70-4.19 μM) and higher selective index (SI: >27.03, >23.87, respectively) against influenza A/WSN/33 virus (H1N1), opening a new direction for quinazoline derivatives in anti-influenza A virus field.
四个含有各种酰胺部分的 2,4-二取代喹唑啉系列化合物被设计和合成，作为使用生物等排和支架跳跃策略的新型抗流感 A 病毒药物。其中许多化合物表现出很强的体外抗流感 A 病毒活性和低细胞毒性（CC: >100 μM）。特别是化合物 10a5 和 17a 对流感 A/WSN/33 病毒（H1N1）表现出更好的活性（IC: 3.70-4.19 μM）和更高的选择指数（SI: >27.03、>23.87，分别），为喹唑啉衍生物在抗流感 A 病毒领域开辟了新的方向。
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