Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Design, Synthesis and Evaluation of Novel 2-piperidinyl Quinoline Chalcones/ Amines as Potential Antidepressant Agents

Author(s): Obaid Afzal, Sandhya Bawa, Suresh Kumar, Rajiv Kumar, Md Quamrul Hassan.

Abstract:

A novel series of 2-piperidinyl quinoline chalcones/amines (3-21) as structural analogues of quipazine were designed in order to find a promising candidate having antidepressant potential. They were synthesized, characterized and screened in vivo for their antidepressant potential by two behavioural models viz. forced swim test (FST) and learned helplessness test (LST). FST showed that compound 5, 8 and 17 reduced significantly the duration of immobility at 20 mg/kg, when compared with the control (p<0.001), and demonstrated comparable activity to clomipramine (p<0.001). LST further supported the antidepressant potential of these compounds. Furthermore, in 5-HTP-induced head-twitch test and yohimbine-induced mortality test, most active compound 5 increased the rate of head-twitching and the prevalence of mortality. Thus, the mechanism of action of the antidepressant effects of compound 1-(2,4-Dichlorophenyl)-3-[2- (piperidin-1-yl) quinolin-3-yl] prop-2-en-1-one (5) may be attributed to increased 5HT and NE level in the synapse.

Keywords: Antidepressant behavioral test, Chalcone, 5-HTP induced mouse head-twitch test, Molinspiration, 2-Piperidinyl quinoline, Quipazine, Reductive amination, Schiff’s base, Yohimbine toxicity potentiation test, catecholamines

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Article Details

VOLUME: 10
ISSUE: 1
Year: 2013
Page: [75 - 85]
Pages: 11
DOI: 10.2174/1570180811309010075