Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers

Title
Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers
Authors
박정은지완근장재완배애님최기현최기항강재효노은주
Keywords
t-type calcium channel; virtual screening; neuropathic pain; focused library
Issue Date
2013-03
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 23, NO 6, 1887-1890
Abstract
To obtain selective and potent inhibitor for T-type calcium channel by ligand based drug design, 2- hydroxy-3-phenoxypropyl piperazine derivatives were synthesized and evaluated for in vitro activities. Compound 6m and 6q showed high selectivity over hERG channel (IC50 ratio of hERG/α1G 6m = 8.5, 6q = 18.38) and they were subjected to measure pharmacokinetics profiles. Among them compound 6m showed an excellent pharmacokinetic profile in rats.
URI
http://pubs.kist.re.kr/handle/201004/44599
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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