Design, Synthesis, and Biological Activity of Chalcone Analogs Containing 4-Phenylquinolin and Benzohydrazide
Design, Synthesis, and Biological Activity of Chalcone Analogs Containing 4-Phenylquinolin and Benzohydrazide
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DOI：
10.1002/cbdv.202100610
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发表时间：
2022-01-27
影响因子：
2.9
通讯作者：
Wang，Si-Hong
中科院分区：
文献类型：
--
作者：
Tan，Qiu-Wan;He，Li-Ya;Wang，Si-Hong
A series of chalcone derivatives (3a–3m) containing 4‐phenylquinoline and benzohydrazide were designed and synthesized, and their anti‐inflammatory, analgesic, and antidepressant activities were evaluated. Using the classic antidepressant model, except for compounds3aand3d, 11 compounds all showed certain antidepressant activity at a dose of 100 mg/kg, among which compounds3f,3h, and3mshowed good antidepressant activity (inhibition rate, respectively 63.0 %, 73.2 %, and 76.4 %), which was equivalent to the positive control fluoxetine (inhibition rate of 70.0 %). Secondly, the inhibitory activity of these compounds on mouse MAOAwas evaluated. At 10 mM, compounds3fand3jshowed a certain selective inhibitory effect on mouse MAOA, while compounds3b,3d,3g,3i, and3mhad a good inhibitory effect on mouse MAOA(inhibition rate is 42.3–71.4 %). The mouse ear edema model was used to evaluate the anti‐inflammatory activity of compounds3a–3m. At 30 mg/kg, compounds3b,3c,3e,3f,3g, and3mshowed certain anti‐inflammatory effects (inhibition rate of 51.5–99.9 %), which was equivalent to the positive control indomethacin (inhibition rate of 69.7 %). Results of the acetic acid‐induced abdominal writhing test showed that, at 30 mg/kg, excepted for compounds3a,3band3d, all the other 10 compounds can show certain analgesic activity (inhibition rate 67–99.9 %). The use of Auto dock Vina (simina) to simulate molecular target docking shows that the development of quinoline and benzohydrazide groups is of great significance to MAOAinhibitors.
