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

Authors
Lee, Jie EunKoh, Hun YeongSeo, Seon HeeBaek, Yi YeonRhim, HyewhonCho, Yong SeoChoo, HyunahPae, Ae Nim
Issue Date
2010-07-15
Publisher
Pergamon Press Ltd.
Citation
Bioorganic & Medicinal Chemistry Letters, v.20, no.14, pp.4219 - 4222
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 mu M, which is comparable with that of mibefradil. (C) 2010 Elsevier Ltd. All rights reserved.
Keywords
NEUROPATHIC PAIN; CA2+ CHANNELS; INHIBITION; NEURONS; NEUROPATHIC PAIN; CA2+ CHANNELS; INHIBITION; NEURONS; T-type calcium channel; HTS assay; alpha(1G) Subtype; Neuropathic pain; Oxazole
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/131250
DOI
10.1016/j.bmcl.2010.05.030
Appears in Collections:
KIST Article > 2010
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