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

Authors
Park, Jung-eun; Ji, Wan Keun; Jang, Jae Wan; Pae, Ae Nim; Choi, Keehyun; Choi, Ki Hang; Kang, Jahyo; Roh, Eun Joo
Issue Date
2013-03-15
Publisher
Pergamon Press Ltd.
Citation
Bioorganic & Medicinal Chemistry Letters, v.23, no.6, pp.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/alpha(1G) 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. (C) 2013 Elsevier Ltd. All rights reserved.
Keywords
CA2+ CHANNELS; INHIBITION; TARGETS; CA2+ CHANNELS; INHIBITION; TARGETS; t-type calcium channel; virtual screening; neuropathic pain; focused library
ISSN
0960-894X
URI
https://pubs.kist.re.kr/handle/201004/128247
DOI
10.1016/j.bmcl.2012.12.072
Appears in Collections:
KIST Article > 2013
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