Literature

Abstract

We designed and synthesized 18 substituted indole derivatives containing a triazole scaffold as novel anti-influenza A virus candidates using a bio-isosteric and scaffold-hopping strategy from the lead compound 4-32-2. Most of the target compounds (eg: 6, 7a, 7d, 7f-j, 7l, 7m, 7o, 7q) exhibited potent anti-influenza A virus activity and low cytotoxicity in vitro. In particular, 7a exhibited the most potent anti-IAV activity (IC<sub>50</sub>: 1.34 ± 0.13 μM) with low cytotoxicity (CC<sub>50</sub>: > 100 μM), and high selectivity index (SI: > 74.63), which provides a new chemical scaffold for the development of novel anti-IAV drug.

DOI： 10.1016/j.bmcl.2022.128681

Design, synthesis, and anti-influenza A virus activity evaluation of novel indole containing derivatives of triazole

Bioorganic & Medicinal Chemistry Letters 2022.0

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

Bioorganic & Medicinal Chemistry Letters 2020.0

Design, Synthesis, and in Vitro Biological Evaluation of 1H-1,2,3-Triazole-4-carboxamide Derivatives as New Anti-influenza A Agents Targeting Virus Nucleoprotein

Journal of Medicinal Chemistry 2012.0

Design, synthesis and in vitro anti-influenza A virus evaluation of novel quinazoline derivatives containing S-acetamide and NH-acetamide moieties at C-4

European Journal of Medicinal Chemistry 2020.0

Synthesis and biological evaluation of novel bisheterocycle-containing compounds as potential anti-influenza virus agents

Bioorganic & Medicinal Chemistry Letters 2005.0

Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus