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Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers |
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| Authors: | Jung-eun Park Wan Keun Ji Jae Wan Jang Ae Nim Pae Keehyun Choi Ki Hang Choi Jahyo Kang Eun Joo Roh |
| Institution: | 1. Chemical Kinomics Research Center, Korea Institute of Science and Technology, Wolsong-gil 5, Seongbuk-gu, Seoul, Republic of Korea;2. Department of Chemistry, Sogang University, Baekbeomno 35, Mapo-gu, Seoul, Republic of Korea;3. Department of Chemistry, Korea University, Anam-dong, Seongbuk-gu, Seoul, Republic of Korea;4. Center for Neuro-Medicine, Korea Institute of Science and Technology, Wolsong-gil 5, Seongbuk-gu, Seoul, Republic of Korea |
| 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. |
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