Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers
- Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers
- 박정은; 지완근; 장재완; 배애님; 최기현; 최기항; 강재효; 노은주
- t-type calcium channel; virtual screening; neuropathic pain; focused library
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 23, NO 6, 1887-1890
- 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.
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