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Design, synthesis, and antidepressant/anticonvulsant activities of 3H-benzo[f]chromen chalcone derivatives
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2021-05-24 , DOI: 10.1007/s00044-021-02742-5
Qiu-Wan Tan , Li-Ya He , Zhi-Wen He , Wei-Hua Liu , Shan-Shan Zhang , Lin Lin , Hong-Li Yang , Li-Ping Guan

In this study, 19 3H-benzo[f]chromen chalcone derivatives (2a2s) were obtained from 2-hydroxy-1-naphthaldehyde as the starting material, and their structures were confirmed by IR, 1H NMR, 13C NMR, and ESI-MS analyses. The antidepressant activities of the compounds were evaluated in mice after one 30 mg/kg dose by means of forced swimming tests, and 18 of the compounds (2a2l, 2n2s) showed antidepressant activity, of which three (2b, 2d, and 2n) showed strong antidepressant activity. Furthermore, all the compounds showed some anticonvulsant activity, with 11 of the compounds (2a2g, 2k, 2m, 2n, and 2q) inhibiting convulsions in the maximal electroshock seizure (MES) test after one dose of 100 mg/kg, and the other eight inhibiting convulsions in the MES after one dose of 300 mg/kg. In the tail suspension test, all the compounds did not show neurotoxicity at the same dose. This research provides an experimental theoretical basis for finding new antidepressants with high biological activity and few side effects.



中文翻译:

3H-苯并[f]铬烯查尔酮衍生物的设计,合成及抗抑郁/抗惊厥活性

在这项研究中,以2-羟基-1-萘甲醛为起始原料,获得了19 3 H-苯并[ f ]铬查尔酮衍生物(2a2s),并通过IR,1 H NMR,13 C NMR证实了其结构。,以及ESI-MS分析。在一剂30 mg / kg的剂量下通过强迫游泳试验对这些化合物的抗抑郁活性进行了评估,其中18种化合物(2a - 2l2n - 2s)具有抗抑郁活性,其中3种(2b2d3d)具有抗抑郁活性。和2n)表现出很强的抗抑郁活性。此外,所有化合物均显示出一定的抗惊厥活性,其中一种化合物(2a - 2g2k2m2n2q)在一次100 mg / kg的最大电击癫痫发作(MES)试验中能抑制惊厥。一剂300 mg / kg剂量后,其他八种抑制MES的惊厥。在尾部悬吊试验中,所有化合物在相同剂量下均未显示神经毒性。该研究为寻找具有高生物活性且副作用少的新型抗抑郁药提供了实验理论依据。

更新日期:2021-05-25
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