Design, Synthesis, Pharmacological Evaluation and Descriptor Based Similarities Study of N,N-diphenyl-2-[4-(substituted phenyl)piperazin-1-yl]acetamides as Potential Antipsychotics

被引：0

作者：

Dash, Radha Charan ^{[1
]}

Bhosale, Sharad H. ^{[1
]}

Shelke, Suhas M. ^{[1
]}

Suryawanshi, Mugdha R. ^{[1
]}

Mahadik, Kakasaheb R. ^{[1
]}

机构：

[1] Bharati Vidyapeeth Deemed Univ, Poona Coll Pharm, Dept Pharmaceut Chem, Pune 411038, Maharashtra, India

来源：

MEDICINAL CHEMISTRY | 2012年 / 8卷 / 06期

关键词：

Antipsychotic; catalepsy; climbing behavior; head twitches; N; N-diphenyl-2-[4-(substituted phenyl)piperazin-1-yl)acetamides; similarities study; CLOZAPINE;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel N,N-diphenyl-2-[4-(substituted phenyl)piperazin-1-yl]acetamides was designed, synthesized and evaluated for anti-dopaminergic activity, anti-serotonergic activity and catalepsy induction studies in mice as an approach to novel potential antipsychotic agent. Antipsychotic activity of these compounds in terms of blocking of dopaminergic transmission was evaluated by their ability to inhibit apomorphine induced climbing behavior in mice and anti-serotonergic activity of synthesized compounds was assessed by studying inhibition of 5-HTP induced head twitches. All the synthesized compounds were found to exhibit anti-dopaminergic and anti-serotonergic activity in behavioral models. The compound 3f showed better antipsychotic potential among the different synthesized compounds. The descriptor based similarities study for blood brain permeation established a good similarity between the synthesized compounds with standard atypical antipsychotics.

引用

页码：1069 / 1075

页数：7

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