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Quinazolindione derivatives as potent 5-HT3A receptor antagonists.

Abstract：

:5-HT(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(3A) receptor antagonists, we screened our in-house small molecule library, resulting in identifying the quinazolindione derivatives as potent 5-HT(3A) receptor antagonists. For the purpose of structure-activity relationship study, 24 quinazolindione analogues were biologically evaluated against 5-HT(3A) receptor. Among those, KKHT10612 shows the best antagonistic effect against 5-HT(3A) receptor with an IC(50) value of 0.8 microM which is comparable with that of the reference compound, MDL72222, and selectivity over T-type calcium channel as well.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Lee BH,Choi MJ,Jo MN,Seo HJ,Nah SY,Cho YS,Nam G,Pae AN,Rhim H,Choo H

doi

10.1016/j.bmc.2009.04.029

subject

Has Abstract

pub_date

2009-07-01 00:00:00

pages

4793-6

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00389-7

journal_volume

17

pub_type

杂志文章

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