Design, synthesis, and antidepressant/anticonvulsant activities of 3H-benzo[f]chromen chalcone derivatives

Article abstract of DOI:10.1007/s00044-021-02742-5

In this study, 19 3H-benzo[f]chromen chalcone derivatives (2a–2s) 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 (2a–2l, 2n–2s) 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 (2a–2g, 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.