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

Oxazole derivatives as T-type calcium channel blockers were synthesized and their biological results were reported. 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 poten...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-07, Vol.20 (14), p.4219-4222
Main Authors: Lee, Jie Eun, Koh, Hun Yeong, Seo, Seon Hee, Baek, Yi Yeon, Rhim, Hyewhon, Cho, Yong Seo, Choo, Hyunah, Pae, Ae Nim
Format: Article
Language:English
Subjects:
Biological and medical sciences
Calcium Channel Blockers - chemical synthesis
Calcium Channel Blockers - pharmacology
Calcium Channels, T-Type - drug effects
Cardiovascular system
Drug Evaluation, Preclinical
HTS assay
Medical sciences
Miscellaneous
Neuropathic pain
Oxazole
Oxazoles - pharmacology
Pharmacology. Drug treatments
T-type calcium channel
α1G Subtype
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Summary:Oxazole derivatives as T-type calcium channel blockers were synthesized and their biological results were reported. 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 α1G (CaV3.1) T-type calcium channel. Among total 41 oxazole compounds synthesized, the most active one was the compound 10-35 with an IC50 value of 0.65μM, which is comparable with that of mibefradil.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.05.030