Park, Jung-eun Ji, Wan Keun Jang, Jae Wan Pae, Ae Nim Choi, Keehyun Choi, Ki Hang Kang, Jahyo Roh, Eun Joo 2024-01-20T12:34:27Z 2024-01-20T12:34:27Z 2021-09-01 2013-03-15 0960-894X https://pubs.kist.re.kr/handle/201004/128247 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. English Pergamon Press Ltd. CA2+ CHANNELS INHIBITION TARGETS Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers Article 10.1016/j.bmcl.2012.12.072 1 Bioorganic & Medicinal Chemistry Letters, v.23, no.6, pp.1887 - 1890 Bioorganic & Medicinal Chemistry Letters 23 6 1887 1890 scie scopus 000315331500065 2-s2.0-84874654558 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article CA2+ CHANNELS INHIBITION TARGETS t-type calcium channel virtual screening neuropathic pain focused library