NISCAIR Online Periodicals Repository

Research Journals >
Indian Journal of Chemistry -Section B (IJC-B) >
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
Sati, Nitin
Veer, V S
Bhosale, S H
Bodhankar, S L
Mahadik, K R
Kadam, S S
Keywords: Substituted methylchromenones
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]

Files in This Item:

File Description SizeFormat
IJCB 44B(11) 2295-2300.pdf145.84 kBAdobe PDFView/Open
 Current Page Visits: 958 
Recommend this item


Online Submission of Articles |  NISCAIR Website |  National Knowledge Resources Consortium |  Contact us |  Feedback

Disclaimer: NISCAIR assumes no responsibility for the statements and opinions advanced by contributors. The editorial staff in its work of examining papers received for publication is helped, in an honorary capacity, by many distinguished engineers and scientists.

CC License Except where otherwise noted, the Articles on this site are licensed under Creative Commons License: CC Attribution-Noncommercial-No Derivative Works 2.5 India

Copyright © 2015 The Council of Scientific and Industrial Research, New Delhi. All rights reserved.

Powered by DSpace Copyright © 2002-2007 MIT and Hewlett-Packard | Compliant to OAI-PMH V 2.0

Home Page Total Visits: 164459 since 01-Sep-2015  Last updated on 21-Jun-2016Webmaster: