Details

Autor(en) / Beteiligte

• Wang, Minghua
• Zhang, Guoning
• Wang, Yujia
• Wang, Juxian
• Zhu, Mei
• Cen, Shan
• Wang, Yucheng

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2020-06, Vol.30 (11), p.127143-127143, Article 127143

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2020

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• Four 2,4-disubstituted quinazoline series containing various amide moieties were designed and synthesized. 10a5 and 17a show better activity (IC50: 3.70–4.19 μM) against IAV A/WSN/33 (H1N1). [Display omitted] 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.