| 张鹏,陈佳林,安巧,邹吉斌,张吉,胡占兴,郝小江.化学通报,2023,86(2):222-232,243. |
| 4H-3,1-苯并噁嗪-4-酮衍生物的合成及α-葡萄糖苷酶抑制活性研究 |
| Synthesis and α-Glucosidase Inhibitory Activities of4H-3, 1-benzoxazine-4-one Derivatives |
| 投稿时间：2022-07-20 修订日期：2022-08-02 |
| DOI： |
| 中文关键词: 4H-3,1-苯并噁嗪-4-酮 α-葡萄糖苷酶抑制剂 分子对接 糖尿病 |
| 英文关键词:4H-3, 1-benzoxazine-4-one, α-glucosidase inhibitor, molecular docking, diabetes mellitus |
| 基金项目:国家自然科学基金项目(U1812403,32160103)和贵州省科学技术厅项目(QKHJC-[2020]-1Y398,QKHZC-[2021]-YB181)资助 |
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| 中文摘要: |
| 为了寻找高效低毒的新型α-葡萄糖苷酶抑制剂,设计并合成了一系列4H-3,1-苯并噁嗪-4-酮衍生物,衍生物结构经过1H NMR、13C NMR和HRMS鉴定。体外α-葡萄糖苷酶抑制活性测定结果表明,化合物3a、4a、5a和4j的IC50值分别为68.3 μM、76.1 μM、99.3 μM和51.9 μM,明显优于阳性对照阿卡波糖(IC50=421.7 μM)。此外,分子对接研究结果表明化合物3a和4j与α-葡萄糖苷酶存在较强的亲和力。 |
| 英文摘要: |
| In order to find novel α-glucosidase inhibitors with high efficiency and low toxicity, a series of 4H-3,1-benzoxazin-4-one derivatives were designed and synthesized. Their structures were elucidated by comprehensive spectroscopic data analysis (1H NMR, 13C NMR and HRMS). Biological tests indicated that compounds 3a, 4a, 5a and 4j exhibited potent α-glucosidase inhibitory activities with IC50 values of 68.3 μM, 76.1 μM, 99.3 μM, and 51.9 μM respectively, which were significantly higher than the positive control acarbose (IC50= 421.7 μM). The results of the molecular docking studies for 3a and 4j with α-glucosidase (PDB codes: 3A4A and 5NN8) showed that compounds 3a and 4j had partially interacted with α-glucosidase. |
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