Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers.
Bioorganic & medicinal chemistry letters 2010 Jul 15; 20(14):4219-22
Lee J JE, Koh H HY, Seo S SH, Baek Y YY, Rhim H, Cho Y YS, Choo H, Pae A AN
Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
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.
Keywords: T-type calcium channel mibefradil