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.

• Authors: Jie Eun Lee, Hun Yeong Koh, Seon Hee Seo, Yi Yeon Baek, Hyewhon Rhim, Yong Seo Cho, Hyunah Choo, Ae Nim Pae
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 14 Pg. 4219-22 (Jul 15 2010) ISSN: 1464-3405 [Electronic] England
• PMID: 20621730 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: 2010 Elsevier Ltd. All rights reserved.

Chemical References

• Calcium Channel Blockers
• Calcium Channels, T-Type
• Oxazoles

Topics

• Calcium Channel Blockers (chemical synthesis, pharmacology)
• Calcium Channels, T-Type (drug effects)
• Drug Evaluation, Preclinical
• Oxazoles (pharmacology)