title: Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers.
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.
authors: Chemical Kinomics Research Center, Korea Institute of Science and Technology, Wolsong-gil 5, Seongbuk-gu, Seoul, Republic of Korea.
authors: Jung-Eun
authors: JE
authors: Park
authors: Wan Keun
authors: WK
authors: Ji
authors: Jae Wan
authors: JW
authors: Jang
authors: Ae Nim
authors: AN
authors: Pae
authors: Keehyun
authors: K
authors: Choi
authors: Ki Hang
authors: KH
authors: Choi
authors: Jahyo
authors: J
authors: Kang
authors: Eun Joo
authors: EJ
authors: Roh
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D020747:Calcium Channels, T-Type / Q000737:chemistry* / Q000378:metabolism; D057809:HEK293 Cells; D006207:Half-Life; D006801:Humans; D000077489:Piperazine; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D010879:Piperazines; D000077489:Piperazine