Design, synthesis, and anti-influenza A virus activity evaluation of novel indole containing derivatives of triazole.
Ji K, Zhang GN, Zhao JY, Zhu M, Wang MH, Wang JX, Cen S, Wang YC, Li WY.
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.