Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines

A series of novel arylpiperazines were synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced climbing behavior (D2antagonism), 5-HTP induced head twitches (5-HT2Aantagonism) and catalepsy studies in albino mice. The physicochemical similarity of the target compounds with respect to standard drugs clozapine, ketanserine and risperidone was assessed by calculating from a set of physiochemical properties using software programs. The test compounds(3a-j)demonstrated good similarity values with respect to the standard drugs. Among them, compound3dhas emerged as an important lead compound showing potential atypical antipsychotic like profile.

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NEW 7-(2-(BENZOL[d]THIAZOL-2-YLAMINO)ETHOXY)-4-METHYL-2HCHROMEN-2-0NE DERIVATIES WITH ATYPICAL ANTIPSYCHOTIC ACTIVITY

Southern Brazilian Journal of Chemistry - Southern Brazilian Journal of Chemistry, Volume 28, No. 28, 2020 ◽

10.48141/sbjchem.v21.n21.2013.95_revista2013.pdf ◽

2013 ◽

Vol 21 (21) ◽

pp. 97-108

Author(s):

Gawai ASHISH ◽

Das SANJIB ◽

Yasbwant PATHAK

Keyword(s):

Atypical Antipsychotic ◽

Dopamine D2 Receptor ◽

Analytical Data ◽

D2 Receptor ◽

Antipsychotic Agents ◽

Antagonistic Activity ◽

High Potency ◽

Climbing Behavior ◽

Head Twitches ◽

Antipsychotic Activity

A new series of 7-(2-(benzo[d]thiazol-2-ylamino)ethoxy)-4-methyl-2H-chromen-2-one derivatives(4a4k) was synthesized and evaluated for their D2 and 51HT2 antagonistic activity as a measure of atypical antipsychotic properly. Compounds 7-(2-(benzo[d]thiazo/-2-ylamino)ethoxy)-4-methyl-2H-chromen-2- one derivatives (4a-4k) was synthesized by refluxing 2-amino benzothiazoles substituted derivatives (3a3k) and 7-(2-Chloroethoxy)-4-melhyl-2H-chromen-2-one (2) in dry pyridine. The synthesized compounds were characterized with the help of spectral and analytical data. Most of these compounds showed dopamine D2 receptor antagonistic activity from moderate to high potency along with serotonin 5-HT2 receptor blockage activity: a property that has been suggested to be necessary for the atypical nature of antipsychotic agents. The D2 and 5-HT2 receptor blockage activity was evaluated by inhibition of apomorphine-induced climbing behavior and 5HTP induced head twitches in mice respectively.

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Synthesis, computational studies and preliminary pharmacological evaluation of 2–[4-(aryl substituted) piperazin-1-yl] N, N-diphenylacetamides as potential antipsychotics

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2011.07.028 ◽

2011 ◽

Vol 46 (9) ◽

pp. 4753-4759 ◽

Cited By ~ 5

Author(s):

Sushil Kumar ◽

A.K. Wahi ◽

Ranjit Singh

Keyword(s):

Computational Studies ◽

Pharmacological Evaluation

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The antipsychotic activity of alcoholic extract of Withania coagulans fruits in Swiss albino mice

International Journal of Basic & Clinical Pharmacology ◽

10.18203/2319-2003.ijbcp20184852 ◽

2018 ◽

Vol 7 (12) ◽

pp. 2389

Author(s):

Amit S. Kamdi ◽

Sarika D. Kokane ◽

Pankaj N. Bohra ◽

Suvarna M. Kalambe

Keyword(s):

Avoidance Response ◽

Conditioned Avoidance ◽

Conditioned Avoidance Response ◽

P Value ◽

Alcoholic Extract ◽

Swiss Albino Mice ◽

Withania Coagulans ◽

Antipsychotic Activity ◽

Albino Mice ◽

Cns Effects

Background: Schizophrenia is one of the most distressing central nervous system (CNS) disorders. It is described by positive, negative and cognitive symptoms. These symptoms can be controlled by the antipsychotic medicines. The numerous antipsychotic medications used today are not lacking the adverse drug reactions. The Withania coagulans a susceptible species, is not explored much for its CNS effects except in late seventies. Therefore, it was thought worthwhile to investigate anti-psychotic activities of alcoholic extract of Withania coagulans fruits. The objective of the present study was to assess the antipsychotic activity of alcoholic extract of Withania coagulans fruits in Swiss albino mice by Cook’s Pole Climb Apparatus for conditioned avoidance response (CAR)Methods: Cook’s Pole Climb Apparatus for conditioned avoidance response was used for assessing the antipsychotic activity of the alcoholic extract of 200mg/kg, 500mg/kg and 1000mg/kg doses of Withania coagulans fruits.Results: There was statistically (p-value >0.05) no significant association between any of the 200mg/kg, 500mg/kg and 1000mg/kg doses of the alcoholic extracts of Withania coagulans fruits with antipsychotic activity in Swiss albino mice.Conclusions: Withania coagulans fruits alcoholic extract did not demonstrate antipsychotic activity in Swiss albino mice under standard conditions.

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