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Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers.

Abstract：

:T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives substituted with arylpiperazinylalkylamines. The oxazoles were synthesized in a convenient convergent synthetic method, and biologically evaluated against alpha(1G) (Ca(V)3.1) T-type calcium channel. Among total 41 oxazole compounds synthesized, the most active one was the compound 10-35 with an IC(50) value of 0.65 microM, which is comparable with that of mibefradil.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lee JE,Koh HY,Seo SH,Baek YY,Rhim H,Cho YS,Choo H,Pae AN

doi

10.1016/j.bmcl.2010.05.030

subject

Has Abstract

pub_date

2010-07-15 00:00:00

pages

4219-22

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00671-2

journal_volume

20

pub_type

杂志文章

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