Title of article
Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers
Author/Authors
Hyewhon Rhim، نويسنده , , Yong Sup Lee، نويسنده , , Seong Jun Park، نويسنده , , Bong Young Chung، نويسنده , , Jae Yeol Lee، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
4
From page
283
To page
286
Abstract
We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca2+ channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca2+ channels and N-type Ca2+ channels. Among them, 5b (KYS05044, IC50 = 0.56 ± 0.10 μM) was identified as potent T-type Ca2+ channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI = >100).
Keywords
3 , 4-Dihydroquinazolines , Channel selectivity , blockers , T-type Ca2+ channel , mibefradil
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795193
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