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; Ki Hang Choi; Jahyo Kang; Eun Joo Roh

doi:10.1016/j.bmcl.2012.12.072

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, Ki Hang Choi, Jahyo Kang, Eun Joo Roh

Research output: Contribution to journal › Article › peer-review

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/α_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.

Original language	English
Pages (from-to)	1887-1890
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	23
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2012.12.072
Publication status	Published - 2013 Mar 15

Bibliographical note

Funding Information:
We thank Medifron DBT for pain animal test. This work was supported by the research fund of Korea Institute of Science and Technology ( 2E 22760 ).

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2012.12.072

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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/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.",

author = "Park, {Jung Eun} and Ji, {Wan Keun} and Jang, {Jae Wan} and Pae, {Ae Nim} and Keehyun Choi and Choi, {Ki Hang} and Jahyo Kang and Roh, {Eun Joo}",

note = "Funding Information: We thank Medifron DBT for pain animal test. This work was supported by the research fund of Korea Institute of Science and Technology ( 2E 22760 ). ",

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AU - Park, Jung Eun

AU - Ji, Wan Keun

AU - Jang, Jae Wan

AU - Pae, Ae Nim

AU - Choi, Keehyun

AU - Choi, Ki Hang

AU - Kang, Jahyo

AU - Roh, Eun Joo

N1 - Funding Information: We thank Medifron DBT for pain animal test. This work was supported by the research fund of Korea Institute of Science and Technology ( 2E 22760 ).

PY - 2013/3/15

Y1 - 2013/3/15

N2 - 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.

AB - 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.

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

Abstract

Bibliographical note

ASJC Scopus subject areas

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