2. Academic Validation
  3. Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers

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.
Jie Eun Lee 1,  Hun Yeong Koh,  Seon Hee Seo,  Yi Yeon Baek,  Hyewhon Rhim,  Yong Seo Cho,  Hyunah Choo,  Ae Nim Pae
Affiliations

Affiliation

  • 1 Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
PMID: 20621730 DOI: 10.1016/j.bmcl.2010.05.030
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.

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