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

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. Copyright © 2022 Elsevier Ltd. All rights reserved.

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Kai Ji, Guo-Ning Zhang, Jian-Yuan Zhao, Mei Zhu, Ming-Hua Wang, Ju-Xian Wang, Shan Cen, Yu-Cheng Wang, Wen-Yan Li. Design, synthesis, and anti-influenza A virus activity evaluation of novel indole containing derivatives of triazole. Bioorganic & medicinal chemistry letters. 2022 May 15;64:128681

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PMID: 35304224

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