Design, synthesis and anti-influenza A virus activity of novel 2,4-disubstituted quinazoline derivatives.,Bioorganic & Medicinal Chemistry Letters

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Design, synthesis and anti-influenza A virus activity of novel 2,4-disubstituted quinazoline derivatives.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-03-27 , DOI: 10.1016/j.bmcl.2020.127143
Minghua Wang ₁ , Guoning Zhang ₁ , Yujia Wang ₁ , Juxian Wang ₁ , Mei Zhu ₁ , Shan Cen ₁ , Yucheng Wang ₁

Affiliation

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 (CC50: >100 μM). Particularly, compounds 10a5 and 17a show better activity (IC50: 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.

中文翻译：

新的2,4-二取代喹唑啉衍生物的设计，合成和抗甲型流感病毒活性。

设计并合成了四个包含各种酰胺基团的2,4-二取代喹唑啉系列作为新型抗甲型流感病毒药物，并采用了生物等位基因和支架跳跃的策略。他们中的许多人表现出有效的体外抗甲型流感病毒活性和低细胞毒性（CC50：> 100μM）。特别是化合物10a5和17a对A / WSN / 33流感病毒（H1N1）表现出更好的活性（IC50：3.70-4.19μM）和更高的选择性指数（SI：> 27.03，> 23.87），为喹唑啉开辟了新的方向抗甲型流感病毒领域的衍生物。

更新日期：2020-04-20

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