Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers
- Authors
- Lee, Jie Eun; Koh, Hun Yeong; Seo, Seon Hee; Baek, Yi Yeon; Rhim, Hyewhon; Cho, Yong Seo; Choo, Hyunah; Pae, 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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