Design, synthesis, and anti-influenza A virus activity evaluation of novel indole containing derivatives of triazole. (15th May 2022)

• Record Type: Journal Article
• Authors: Ji, Kai; Zhang, Guo-Ning; Zhao, Jian-Yuan; Zhu, Mei; Wang, Ming-Hua; Wang, Ju-Xian; Cen, Shan; Wang, Yu-Cheng; Li, Wen-Yan
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 64(2022)
• Publication Date: 2022-05-15
• Subjects: Indole containing triazole -- Design -- Synthesis -- Anti-influenza A virus activity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2022.128681
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 (IC50 : 1.34 ± 0.13 μM) with low cytotoxicity (CC50 : > 100 μM), and high selectivity index (SI: > 74.63), which provides a new chemical scaffold for the development of novel anti-IAV drug.