Quinazolindione derivatives as potent 5-HT3A receptor antagonists
- Quinazolindione derivatives as potent 5-HT3A receptor antagonists
- 이병환; 최민정; 조미나; 서희정; 나승렬; 조용서; 남길수; 배애님; 임혜원; 추현아
- 5-HT3A receptor; antagonist; quinazolindione derivatives; MDL72222; calcium channel; serotonin; Bemesetron
- Issue Date
- Bioorganic & medicinal chemistry
- VOL 17, 4793-4796
- 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.
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