Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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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

Affiliation: Food and Pharmacy College, Zhejiang Ocean University, Zhoushan City, Zhejiang Province, 316022, P.R. China.

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

Graphical Abstract:


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.

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Article Details

VOLUME: 10
ISSUE: 8
Page: [789 - 799]
Pages: 11
DOI: 10.2174/1573406410666140328125641