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Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers.

Abstract：

:We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type Ca(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type Ca(2+) channels and N-type Ca(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type Ca(2+) channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI=>100).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Rhim H,Lee YS,Park SJ,Chung BY,Lee JY

doi

10.1016/j.bmcl.2004.10.078

subject

Has Abstract

pub_date

2005-01-17 00:00:00

pages

283-6

issue

2

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01318-6

journal_volume

15

pub_type

杂志文章

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