Quinazolindione derivatives as potent 5-HT3A receptor antagonists

Title
Quinazolindione derivatives as potent 5-HT3A receptor antagonists
Authors
이병환최민정조미나서희정나승렬조용서남길수배애님임혜원추현아
Keywords
5-HT3A receptor; antagonist; quinazolindione derivatives; MDL72222; calcium channel; serotonin; Bemesetron
Issue Date
2009-06
Publisher
Bioorganic & medicinal chemistry
Citation
VOL 17, 4793-4796
Abstract
5-HT3A receptor antagonists have been used mainly for the treatment of nausea and vomiting. These days, the antagonists are of special interest due to their therapeutic potential to treat other diseases such as depression, psychotic disorder, drug abuse, and irritable bowel syndrome. To discover novel 5-HT3A receptor antagonists, we screened our in-house small molecule library, resulting in identifying the quinazolindione derivatives as potent 5-HT3A receptor antagonists. For the purpose of structure–activity relationship study, 24 quinazolindione analogues were biologically evaluated against 5-HT3A receptor. Among those, KKHT10612 shows the best antagonistic effect against 5-HT3A receptor with an IC50 value of 0.8 lM which is comparable with that of the reference compound, MDL72222, and selectivity over T-type calcium channel as well.
URI
http://pubs.kist.re.kr/handle/201004/35475
ISSN
0968-0896
Appears in Collections:
KIST Publication > Article
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