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

Jung Eun Park, Wan Keun Ji, Jae Wan Jang, Ae Nim Pae, Keehyun Choi, Kihang Choi, Jahyo Kang, Eun Joo Roh

Research output: Contribution to journalArticle

3 Citations (Scopus)

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/α1G 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.

Original languageEnglish
Pages (from-to)1887-1890
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number6
DOIs
Publication statusPublished - 2013 Mar 15

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T-Type Calcium Channels
Pharmacokinetics
Calcium Channel Blockers
Derivatives
Drug Design
Inhibitory Concentration 50
Rats
Ligands
Pharmaceutical Preparations
piperazine

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl) piperazine derivatives as T-type calcium channel blockers. / Park, Jung Eun; Ji, Wan Keun; Jang, Jae Wan; Pae, Ae Nim; Choi, Keehyun; Choi, Kihang; Kang, Jahyo; Roh, Eun Joo.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 6, 15.03.2013, p. 1887-1890.

Research output: Contribution to journalArticle

Park, Jung Eun ; Ji, Wan Keun ; Jang, Jae Wan ; Pae, Ae Nim ; Choi, Keehyun ; Choi, Kihang ; Kang, Jahyo ; Roh, Eun Joo. / Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl) piperazine derivatives as T-type calcium channel blockers. In: Bioorganic and Medicinal Chemistry Letters. 2013 ; Vol. 23, No. 6. pp. 1887-1890.
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