Synthesis and SAR of N-Chlorophenyl Substituted Piperazinylethyl-aminomethylpyrazoles as 5-HT3A Inhibitors

Authors
Lee, Byung-HwanChoi, In SungRhim, HyewhonChoi, Kyung IlNah, Seung-YeolNam, Ghilsoo
Issue Date
2009-11-20
Publisher
KOREAN CHEMICAL SOC
Citation
BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.30, no.11, pp.2707 - 2712
Abstract
he 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-IIT) of a series of pyrazole derivatives having N-chlorophenylpiperazine functionality (6-9). We found that most N-p-chlorophenyl substituted piperazinyl-pyrazole derivatives (7b, 7c, 7e, and 7h) exhibited the high potency for the inhibition of I-5-HT,I- whereas the compound without (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-IIT.
Keywords
RECEPTOR ANTAGONISTS; SEROTONIN; CHANNEL; RECEPTOR ANTAGONISTS; SEROTONIN; CHANNEL; 5-HT3 receptor; 5-HT3A receptor channel activity; Novel 5-HT3 receptor channel current blockers; Chlorophenyl substituted piperazinylethylaminomethylpyrazoles
ISSN
0253-2964
URI
https://pubs.kist.re.kr/handle/201004/131957
Appears in Collections:
KIST Article > 2009
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