Quinazolindione derivatives as potent 5-HT sub(3A) receptor antagonists

Quinazolindione derivatives as potent 5-HT sub(3A) receptor antagonists

5-HT sub(3A) 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 discov...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2009-07, Vol.17 (13), p.4793-4796
Hauptverfasser: Lee, Byung-Hwan, Choi, Min Jung, Jo, Mi Na, Seo, Hee Jeong, Nah, Seung-Yeol, Cho, Yong Seo, Nam, Ghilsoo, Pae, Ae Nim, Rhim, Hyewhon, Choo, Hyunah
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container_end_page 4796
container_issue 13
container_start_page 4793
container_title Bioorganic & medicinal chemistry
container_volume 17
creator Lee, Byung-Hwan
Choi, Min Jung
Jo, Mi Na
Seo, Hee Jeong
Nah, Seung-Yeol
Cho, Yong Seo
Nam, Ghilsoo
Pae, Ae Nim
Rhim, Hyewhon
Choo, Hyunah
description 5-HT sub(3A) 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- HT sub(3A) receptor antagonists, we screened our in-house small molecule library, resulting in identifying the quinazolindione derivatives as potent 5-HT sub(3A) receptor antagonists. For the purpose of structure-activity relationship study, 24 quinazolindione analogues were biologically evaluated against 5-HT sub(3A) receptor. Among those, KKHT10612 shows the best antagonistic effect against 5-HT sub(3A) receptor with an IC sub(50) value of 0.8 mu M which is comparable with that of the reference compound, MDL72222, and selectivity over T-type calcium channel as well.
doi_str_mv 10.1016/j.bmc.2009.04.029
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title Quinazolindione derivatives as potent 5-HT sub(3A) receptor antagonists
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