Design, synthesis and anti-influenza A virus activity of novel 2,4-disubstituted quinazoline derivatives

Bioorg Med Chem Lett. 2020 Jun 1;30(11):127143. doi: 10.1016/j.bmcl.2020.127143.

Minghua Wang ¹, Guoning Zhang ¹, Yujia Wang ¹, Juxian Wang ¹, Mei Zhu ¹, Shan Cen ², Yucheng Wang ³

Affiliations

1 Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.
2 Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China. Electronic address: [email protected].
3 Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China. Electronic address: [email protected].

PMID: 32273213 DOI: 10.1016/j.bmcl.2020.127143

Abstract

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.

Keywords

Anti-influenza A virus activity; Design; Quinazoline derivatives; Synthesis.

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