Referenced in: none

Automatically associated channels: Cav3.1

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

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

Journal, date & volume: Bioorg. Med. Chem. Lett., 2010 Jul 15 , 20, 4219-22

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20621730

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.