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

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

  • Bioorg Med Chem Lett. 2013 Mar 15;23(6):1887-90. doi: 10.1016/j.bmcl.2012.12.072.
Jung-Eun Park 1,  Wan Keun Ji,  Jae Wan Jang,  Ae Nim Pae,  Keehyun Choi,  Ki Hang Choi,  Jahyo Kang,  Eun Joo Roh
Affiliations

Affiliation

  • 1 Chemical Kinomics Research Center, Korea Institute of Science and Technology, Wolsong-gil 5, Seongbuk-gu, Seoul, Republic of Korea.
PMID: 23395659 DOI: 10.1016/j.bmcl.2012.12.072
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.

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