2. Academic Validation
  3. Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers

Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers

  • Bioorg Med Chem Lett. 2010 May 1;20(9):2705-8. doi: 10.1016/j.bmcl.2010.03.084.
Su Jin Gu 1,  Jae Kyun Lee,  Ae Nim Pae,  Hye Jin Chung,  Hyewon Rhim,  So Yeob Han,  Sun-Joon Min,  Yong Seo Cho
Affiliations

Affiliation

  • 1 Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongyang, Seoul 130-650, Republic of Korea.
PMID: 20382529 DOI: 10.1016/j.bmcl.2010.03.084
Abstract

We have synthesized and biologically evaluated 1,4-diazepane derivatives as T-type calcium channel blockers. In this study, we discovered compound 4s, a potential T-type calcium channel blocker with good selectivity over hERG and N-type calcium channels. In addition, it exhibited favorable pharmacokinetic characteristics for further investigation of T-type calcium channel related diseases.

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