Synthesis and SAR of N-chlorophenyl substituted piperazinylethyl-aminomethylpyrazoles as 5-HT3A Inhibitors

Title
Synthesis and SAR of N-chlorophenyl substituted piperazinylethyl-aminomethylpyrazoles as 5-HT3A Inhibitors
Authors
이병환최인성임혜원최경일나승렬남길수
Keywords
5-HT3 receptor; 5-HT3 receptor channel activity; 5-HT3 receptor channel current blocker; chlorophenyl substituted pyrazole
Issue Date
2009-11
Publisher
Bulletin of the Korean Chemical Society
Citation
VOL 30, NO 11, 2707-2712
Abstract
The 5-HT3A receptors are one of ligand-gated ion channels and are known to be involved in visceral pain, anxiety, or anticancer agent-induced nausea and vomiting. In present study, we designed novel skeletons based on the developed 5-HT3 receptor antagonists and evaluated their effects on 5-HT3A receptor channel currents (I5-HT) of a series of pyrazole derivatives having N-chlorophenylpiperazine functionality (6-9). We found that most of N-p-chlorophenyl substituted piperazinyl-pyrazole derivatives (7b, 7c, 7e and 7h) exhibited the high potency for the inhibition of I5-HT, whereas the compound without chloride (6) or with m-chlorophenyl group (a serious of 8 and 9) showed the low potency. These results indicate that p-chlorophenyl group is might play an important role for increasing the inhibitory potency on I5-HT.
URI
http://pubs.kist.re.kr/handle/201004/36635
ISSN
0253-2964
Appears in Collections:
KIST Publication > Article
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE