| 刘进兵,唐君源.化学通报,2017,80(1):77-83. |
| 卤代查尔酮氨基硫脲席夫碱的合成及生物活性研究 |
| Bioactivities of chalcones with halogen atoms and their thiosemicarbazide derivatives |
| 投稿时间：2016-05-21 修订日期：2016-06-25 |
| DOI： |
| 中文关键词: 查尔酮衍生物 生物活性 酪氨酸酶抑制机理 分子对接. |
| 英文关键词:chalcone derivatives bioactivity tyrosinase inhibition mechanism docking studies. |
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| 中文摘要: |
| 本文合成了一系列卤代查尔酮及其氨基硫脲席夫碱，并考察了所合成化合物酪氨酸酶抑制活性及抗氧化活性。结果表明：部分化合物具有较好的酪氨酸酶抑制活性，其中3个化合物的抑制活性强于阳性对照曲酸，化合物9（4-溴代查尔酮氨基硫脲席夫碱）表现出最好的抑制活性，其IC50值为2.02 μmol/L；部分化合物还具有一定的抗氧化活性。抑制机理研究表明化合物9属于不可逆抑制剂。优选化合物9进行了分子对接探讨。初步构效关系分析为进一步研究具有酪氨酸酶抑制活性的类似化合物提供了参考。 |
| 英文摘要: |
| A series of halogen atom substituted chalcones and their derivatives were synthesized. All of the compounds were evaluated for their antioxidant activities and inhibitory activities against mushroom tyrosinase. The results showed that some of the synthesized compounds exhibited significant tyrosinase inhibitory activities, three compounds exhibited more potent inhibitory activities than the reference standard inhibitor. Especially, compound 9 exhibited the most potent tyrosinase inhibitory activity with an IC50 value of 2.02 μmol/L. In addition, some compounds showed certain antioxidant activities. The inhibition mechanism analysis of compound 9 showed that the inhibitory effect of the compound on the tyrosinase was irreversible. Preliminary structure activity relationships’ (SARs) analysis suggested that further development of such compounds might be of interest. Docking studies showed sulfur atom and phenyl ring B could form π bond with residue of the tyrosinase, and the amino could form hydrogen bond with HIS178. |
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