Citation: Genqiang Chen, Lina Zhu, Song Zhang, Yuanhao Li, Xiaolong Guo, Zhiping Che. Syntheses and In Vitro Anti-HIV-1 Activities of N-Phenylsulfonyl-3-acetylindole Carbonyl Hydrazone Derivatives[J]. Chemistry, ;2021, 84(5): 467-473. shu

Syntheses and In Vitro Anti-HIV-1 Activities of N-Phenylsulfonyl-3-acetylindole Carbonyl Hydrazone Derivatives

Laboratory of Pharmaceutical Design & Synthesis, Department of Plant Protection, College of Forestry, Henan University of Science and Technology, Luoyang, 471023

Corresponding author: Zhiping Che, zhipingche@163.com; czpgsts@haust.edu.cn
Received Date: 13 October 2020
Accepted Date: 7 December 2020

Figures(2)

As our ongoing work on research of anti-HIV-1 inhibitors, 26 N-phenylsulfonyl-3-acetylindole carbonyl hydrazone derivatives 3a~3z were designed and prepared through a modified route. This procedure imbues the synthetic methodology with green credentials. All the target compounds were also well evaluated for their inhibitory activities against HIV-1 replication in vitro. The results demonstrated that compounds 3a, 3g, 3t and 3w~3y display significant anti-HIV-1 activity. In particular, the N-phenylsulfonyl-3-acetylindole 3-methylbenzoyl hydrazone (3a) and N-(3-nitro) phenylsulfonyl-3-acetyl-6-methylindole 2-thienylformyl hydrazine (3t) exhibit the most potent anti-HIV-1 activity with EC₅₀ values of 0.77 and 0.74 μg/mL, and TI values of >259.74 and >270.27, respectively. Therefore, target compounds 3a and 3t might be identified as the promising candidates for further chemical optimization.
- Indole,
- Carbonyl hydrazine,
- HIV-1,
- Inhibitor of virus replication
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