Facile synthesis and biological evaluation of 3,3-diphenylpropanoyl piperazines as T-type calcium channel blockers

  • Choi, Yeon-hee; 
  • Baek, Du Jong; 
  • Seo, Seon Hee; 
  • Lee, Jae Kyun; 
  • Pae, Ae Nim; 
  • ... Min, Sun-Joon; 
  • 외 1명
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초록

We have developed a facile synthesis of 3,3-diphenylpropanamides using Meldrum's acid derivatives as amide coupling components. The in vitro biological evaluation of the title compounds led to the identification of compound 1h, which has good inhibitory activity against T-type calcium channel (IC50 = 0.83 mu M). (C) 2010 Elsevier Ltd. All rights reserved.

키워드

T-Type calcium channel blockers; Meldrum's acid; 3,3-Diphenylpropanoyl piperazine; HTS assays; MELDRUMS ACIDS; DERIVATIVES; EFFICIENT; ANALOGS
제목
Facile synthesis and biological evaluation of 3,3-diphenylpropanoyl piperazines as T-type calcium channel blockers
저자
Choi, Yeon-hee; Baek, Du Jong; Seo, Seon Hee; Lee, Jae Kyun; Pae, Ae Nim; Cho, Yong Seo; Min, Sun-Joon
DOI
10.1016/j.bmcl.2010.11.033
발행일
2011-01
유형
Article
저널명
Bioorganic & Medicinal Chemistry Letters
권
21
호
1
페이지
215 ~ 219