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

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

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

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4219-22. doi: 10.1016/j.bmcl.2010.05.030. Epub 2010 May 15.

PubMed ID

20621730 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mibefradil	Voltage-dependent T-type calcium channel subunit alpha-1G	IC 50 (nM)	860	N/A	N/A	Details
Mibefradil	Voltage-dependent T-type calcium channel subunit alpha-1G	IC 50 (nM)	830	N/A	N/A	Details