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

Bioorganic & Medicinal Chemistry Letters
2020.0

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 (CC<sub>50</sub>: >100 μM). Particularly, compounds 10a5 and 17a show better activity (IC<sub>50</sub>: 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.

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