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Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Synthesis of 2`-hydroxy-4`-isoprenyloxychalcone Derivatives with Potential Antidepressant-like Activity

Author(s): Chao Xie, Zhou Peng, Shui-Lian Zhao, Cheng-Yan Pan, Li-Ping Guan and Xian-Yu Sun

Volume 10, Issue 8, 2014

Page: [789 - 799] Pages: 11

DOI: 10.2174/1573406410666140328125641

Price: $65

Abstract

A series of 2´-hydroxy-4´-isoprenyloxychalcone derivatives was synthesized and evaluated for its antidepressant- like activity using the FST and TST. All compounds exhibited the potential antidepressant-like activity in the FST and the TST through intraperitoneal injection. Among them, compounds 4i, 4l and 4n exhibited more potent antidepressant- like activity at a dose of 10 mg/kg. And, compounds 4i, 4l and 4n were also adequately absorbed in mice after oral administration at a dose of 30 mg/kg. In the 5-HT induced head-twitch test and yohimbine induced mortality test, compound 4i could increase the head-twitch and rise mortality in mice. The results suggested that the antidepressant effects of compound 4i may be related to via the serotonergic and noradrenergic system.

Keywords: 2´-Hydroxy-4´-isoprenyloxychalcone, synthesis, antidepressant-like activity, yohimbine, 5-hydroxytryptophan.

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