Title:Design, Synthesis, Pharmacological Evaluation and Descriptor Based Similarities Study of N,N-diphenyl-2-[4-(substituted phenyl)piperazin-1- yl]acetamides as Potential Antipsychotics
Volume: 8
Issue: 6
Author(s): Radha Charan Dash, Sharad H. Bhosale, Suhas M. Shelke, Mugdha R. Suryawanshi and Kakasaheb R. Mahadik
Affiliation:
Keywords:
Antipsychotic, catalepsy, climbing behavior, head twitches, N, N-diphenyl-2-[4-(substituted phenyl)piperazin-1-
yl)acetamides, similarities study
Abstract: 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 antiserotonergic
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.