title: 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.affiliation: Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
authors.forename: Jie Eun
authors.initials: JE
authors.lastname: Lee
authors.forename: Hun Yeong
authors.initials: HY
authors.lastname: Koh
authors.forename: Seon Hee
authors.initials: SH
authors.lastname: Seo
authors.forename: Yi Yeon
authors.initials: YY
authors.lastname: Baek
authors.forename: Hyewhon
authors.initials: H
authors.lastname: Rhim
authors.forename: Yong Seo
authors.initials: YS
authors.lastname: Cho
authors.forename: Hyunah
authors.initials: H
authors.lastname: Choo
authors.forename: Ae Nim
authors.initials: AN
authors.lastname: Pae
mesh_terms: D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D020747:Calcium Channels, T-Type / Q000187:drug effects*; D004353:Drug Evaluation, Preclinical; D010080:Oxazoles / Q000494:pharmacology*
chemical_list: D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D010080:Oxazoles