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

…, JW Jang, AN Pae, K Choi, KH Choi, J Kang…

Index: Park, Jung-Eun; Ji, Wan Keun; Jang, Jae Wan; Pae, Ae Nim; Choi, Keehyun; Choi, Ki Hang; Kang, Jahyo; Roh, Eun Joo Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1887 - 1890

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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 ...