DESIGN, SYNTHESIS AND PSYCHOPHARMACOLOGICAL ACTIVITY OF QUINOLIN-2-ONE DERIVATIVES

Starting material 4-hydroxy-1-phenyl/methyl-quinolin-2-(1H)-one was treated with phosphorous oxychloride and then subjected to Mannich reaction to yield title 4-chloro-1-phenyl/methyl-3-[3- (substituted) propanoyl] quinolin-2(1H)-one derivatives compounds IIa (1-7)/ IIb (1-7). Molecular docking studies of the compounds were carried out using Molegro Virtual Docker. All the synthesized compounds were characterized by IR, 1H-NMR and Mass Spectral data and were tested for their antidepressant activity. Amongst the synthesized compounds, compound 4-chloro-1-phenyl-3-[3-(morpholinopropanoyl] quinolin-2(1H)-one [IIa4] was found to show the most potent antidepressant activity with immobility time of 98.17± 4.806. Compound 4-chloro-1-phenyl-3-[3-(4- methylpiperazin-1-yl) propanoyl] quinolin-2(1H)- one [IIa 3] and 4-chloro-1-methyl-3-[3-(pyrrolidin-1-yl) propanoyl] quinolin-2(1H)-one [IIb 2] showed moderate antidepressant activity with immobility time of 126.5 ± 1.945s and 120.3 ± 2.376s, respectively, compared to standard imipramine.

PSYCHOPHARMACOLOGICAL ACTIVITY;

Objective: The purpose of this study was to screen some herbal medicine as psychotropic drugs those has strong modulatingeffect on brain and behavior. Material & methods: Herbal drug Reserpine, Nux- Vomica, Anacardium and Chlorpromazine with a wide range ofpharmacological actions. In our present study, we evaluate the effectiveness of these drugs as Psychotropic agents and accessed bybiochemical-parameters. Rats (weighing 180-250g) and Mice (22-32g) either sex were used in this study. One group was kept as control fordrugs. Mice were kept under room temperature. Tap-water was allowed ad-Libitum. Animals were observed during and after 21 days. A tabletcrushed in 10ml of water, 1cc was given. Screening method used was swimming induced-despair. Results: Among these, Strychnos Nux-Vomica has strong action on cholinergic system, CNS activity and observed as an antispasmodic. Rauwolfia serpentine is an active alkaloidparticularly present in reserpine are used to treat essential hypertension and in certain neuropsychiatry disorders. It has sedative andtranquilizing effects, as it depletes catecholamine from the central nervous system. Keeping in view, the medicinal importance of these herbs,our present study was designed to screen these herbs as for CNS activity on Albino mice and rats.

Synthesis and Analgesic-like Effect of (6R, 4S)-p-Mentha-1,8-dien-6-ylmethylene- p-toluenesulfonamide

The synthesis of a monoterpene-based para-toluenesulfonamide is reported starting from naturally occurring (R)- (−)-carvone (1), by 1,2-addition of HCN followed by reduction with lithium aluminum hydride to afford the amino alcohols 3a and 3b. Tosylation of thismixture with p-toluenesulfonyl chloride furnished sulfonamide 4 in 55% overall yield. Compound 4 was evaluated in behavior animal models to investigate its effects on the central nervous system. It showed low toxicity and sedative action in mice, indicating it to be psychoactive. It also caused a decrease in the spontaneous motor activity of mice. This depressant effect was confirmed in the acetic acid-induced writhing test, which demonstrated a significant antinociceptive response more potent than 1. The present results provide evidence that sulfonamide 4 has analgesic-like psychopharmacological activity.