Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers.
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.
Lee
Jie Eun
JE
Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
Koh
Hun Yeong
HY
Seo
Seon Hee
SH
Baek
Yi Yeon
YY
Rhim
Hyewhon
H
Cho
Yong Seo
YS
Choo
Hyunah
H
Pae
Ae Nim
AN
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*
D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D010080:Oxazoles