Referenced in: none

Automatically associated channels: Kv11.1

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

Authors: Jung-Eun Park, Wan Keun Ji, Jae Wan Jang, Ae Nim Pae, Keehyun Choi, Ki Hang Choi, Jahyo Kang, Eun Joo Roh

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Mar 15 , 23, 1887-90

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23395659

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.