| 陈根强,朱丽娜,张嵩,李元昊,郭小龙,车志平.化学通报,2021,84(5):467-473. |
| N-苯磺酰基-3-乙酰基吲哚羰基酰腙类衍生物合成及其体外抗HIV-1活性研究 |
| Syntheses and In Vitro Anti-HIV-1 Activities of N-Phenylsulfonyl-3-acetylindole Carbonyl Hydrazone Derivatives |
| 投稿时间：2020-10-13 修订日期：2020-12-07 |
| DOI： |
| 中文关键词: 吲哚 羰基酰腙 HIV-1 病毒复制抑制剂 |
| 英文关键词:Indole Carbonyl hydrazine HIV-1 Inhibitor of virus replication |
| 基金项目:国家自然科学基金项目（31901863）资助 |
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| 中文摘要: |
| 基于长期进行的抗HIV-1抑制剂研究，通过优化路线并设计合成了26个N-苯磺酰基-3-乙酰基吲哚羰基酰腙类衍生物（3a~3z）。该方法环保，为今后制备腙类化合物提供了绿色合成途径。所有目标化合物在体外均测定了其对HIV-1抑制活性。结果表明，化合物3a、3g、3t和3w~3y表现出较好的抗HIV-1活性，特别是N-苯磺酰基-3-乙酰基吲哚-3-甲基苯甲酰腙（3a）和N-（3-硝基）-苯磺酰基-3-乙酰基-6-甲基吲哚-2-噻吩甲酰腙（3t）表现出显著的抗HIV-1活性，其对应EC50值分别为0.77和0.74μg/mL，TI值分别为>259.74和>270.27。因此，化合物3a和3t可作为候选化合物经进一步结构优化研究其HIV-1活性。 |
| 英文摘要: |
| 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. |
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