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