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

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

  • Bioorg Med Chem Lett. 2022 May 15:64:128681. doi: 10.1016/j.bmcl.2022.128681.
Kai Ji 1,  Guo-Ning Zhang 2,  Jian-Yuan Zhao 2,  Mei Zhu 2,  Ming-Hua Wang 2,  Ju-Xian Wang 2,  Shan Cen 3,  Yu-Cheng Wang 4,  Wen-Yan Li 5
Affiliations

Affiliations

  • 1 Hebei Key Laboratory of Organic Functional Molecules, College of Chemistry and Materials Science, Hebei Normal University, Shijiazhuang 050024, PR China; Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, PR China.
  • 2 Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, PR China.
  • 3 Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, PR China. Electronic address: [email protected].
  • 4 Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, PR China. Electronic address: [email protected].
  • 5 Hebei Key Laboratory of Organic Functional Molecules, College of Chemistry and Materials Science, Hebei Normal University, Shijiazhuang 050024, PR China. Electronic address: [email protected].
PMID: 35304224 DOI: 10.1016/j.bmcl.2022.128681
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.

Keywords

Anti-influenza A virus activity; Design; Indole containing triazole; Synthesis.

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