Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370380 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
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/α1G6m = 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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jung-eun Park, Wan Keun Ji, Jae Wan Jang, Ae Nim Pae, Keehyun Choi, Ki Hang Choi, Jahyo Kang, Eun Joo Roh,