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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
被引:11
|作者:
Kumar, Sushil
[1
]
Wahi, A. K.
[1
]
Singh, Ranjit
[2
]
机构:
[1] IFTM, Coll Pharm, Drug Design & Med Chem Res Lab, Moradabad 244001, UP, India
[2] Shobhit Univ, Sch Pharmaceut Sci, Meerut, Uttar Pradesh, India
关键词:
N;
N-diphenylacetamide;
Arylpiperazines;
Computational studies;
Antipsychotic activity;
Dopamine and Serotonin antagonists;
RECEPTOR-ACTIVITY;
ARYLPIPERAZINES;
AFFINITY;
5-HT1A;
DERIVATIVES;
CATALEPSY;
ANALOGS;
SERIES;
AGENTS;
DRUGS;
D O I:
10.1016/j.ejmech.2011.07.028
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
A series of 2-[4-(aryl substituted) piperazin-1-yl] N, N-diphenylacetamides have been synthesized and the target compounds (3a-j) were evaluated for atypical antipsychotic activity in apomorphine induced climbing, 5-HTP induced head twitches behavior and catalepsy studies in mice. The physicochemical similarity of the target compounds with respect to standard drugs clozapine, ketanserin and risperidone was calculated by using software programs. Among them, compound 3e showed maximum atypical antipsychotic like profile. (C) 2011 Elsevier Masson SAS. All rights reserved.
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页码:4753 / 4759
页数:7
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