Synthesis and biological activity of 3,4-dihydroquinazolines for selective T-type Ca2+ channel blockers

  • Bioorg Med Chem Lett. 2005 Jan 17;15(2):283-6. doi: 10.1016/j.bmcl.2004.10.078.
Hyewhon Rhim  1 ,  Yong Sup Lee ,  Seong Jun Park ,  Bong Young Chung ,  Jae Yeol Lee
Affiliations
  • 1. Life Sciences Division, Korea Institute of Science & Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
PMID: 15603940 DOI: 10.1016/j.bmcl.2004.10.078
Abstract

We have synthesized 3,4-dihydroquinazoline derivatives for the potent and selective T-type CA(2+) channel blockers and evaluated for their inhibitory activities against two subtypes T-type CA(2+) channels and N-type CA(2+) channels. Among them, 5b (KYS05044, IC(50)=0.56+/-0.10 microM) was identified as potent T-type CA(2+) channel blocker with in vitro selectivity profile at meaningful level (T/N-type, SI=>100).