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

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):215-9. doi: 10.1016/j.bmcl.2010.11.033.
Yeon-hee Choi  1 ,  Du Jong Baek ,  Seon Hee Seo ,  Jae Kyun Lee ,  Ae Nim Pae ,  Yong Seo Cho ,  Sun-Joon Min
Affiliations
  • 1. Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongyang, Seoul 130-650, Republic of Korea.
PMID: 21126876 DOI: 10.1016/j.bmcl.2010.11.033
Abstract

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 (IC(50) = 0.83 μM).