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IJC-B Vol.44B [2005] >
IJC-B Vol.44B(11) [November 2005] >


Title: 7-[(4-Substituted phenyl-piperazin-1-yl)-alkoxyl]-4-methylchromene-2-ones as potential atypical antipsychotics: Synthesis and pharmacological evaluation
Authors: Shelke, S M
Sushilkumar
Sati, Nitin
Veer, V S
Bhosale, S H
Bodhankar, S L
Mahadik, K R
Kadam, S S
Keywords: Substituted methylchromenones
antipsychotics
pharmacological evaluation
dichlorophenyl piperazines
Issue Date: Nov-2005
Publisher: CSIR
IPC CodeInt.Cl.7 C 07 D // A 61 P/28
Abstract: 7-Hydroxy-4-methylchromene-2-one 1 when reacted respectively with 2-bromo-1-chloroethane and 3-bromo-1-chloropropane in acetonitrile and in the presence of anhydrous K2CO3 yields 7-alkoxy-4-methylchromene-2-ones 2a,b. Compounds 2a,b when refluxed with various arylpiperazines in toluene and in the presence of triethylamine yield the title compounds, 7-[(4-substituted phenyl-piperazin-1-yl)-alkoxyl]-4-methylchromen-2-ones 3a-j.Their atypical antipsychotic activity have been evaluated by their ability to inhibit apomorphine induced climbing behavior (D2 antagonism) and to inhibit the 5–HTP induced head twitches in albino mice (5-HT2A antagonism) alongwith catalepsy studies. All the compounds inhibit apomorphine induced climbing behavior and 5-HTP induced head twitches. The SAR studies reveal that methyl group in the phenyl ring of piperazine and the chain length (n=3) gives more dopaminergic and serotonergic antagonistic activity, while dichlorophenyl piperazines have less dopaminergic and serotonergic antagonistic activity. 3f and 3g have been found to have significant atypical behaviour.
Page(s): 2295-2300
ISSN: 0975-0983(Online); 0376-4699(Print)
Source:IJC-B Vol.44B(11) [November 2005]

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