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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, Ki Hang;
- 외 2명
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3초록
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/alpha(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. (C) 2013 Elsevier Ltd. All rights reserved.
키워드
CA2+ CHANNELS; INHIBITION; TARGETS
- 제목
- Synthesis and biological evaluation of 1-(2-hydroxy-3-phenyloxypropyl)piperazine derivatives as T-type calcium channel blockers
- 저자
- Park, Jung-eun; Ji, Wan Keun; Jang, Jae Wan; Pae, Ae Nim; Choi, Keehyun; Choi, Ki Hang; Kang, Jahyo; Roh, Eun Joo
- 발행일
- 2013-03-15
- 유형
- Article
- 권
- 23
- 호
- 6
- 페이지
- 1887 ~ 1890
- 언어
- ENG
- 출판사
- PERGAMON-ELSEVIER SCIENCE LTD
- 발행국가
- 영국
- 분량
- 4 페이지
- ISSN
- E 1464-3405
P 0960-894X