Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Synthesis and Biological Evaluation of 1-Heteroarylmethyl 1,4-Diazepanes Derivatives as Potential T-type Calcium Channel Blockers

  • Ullapu, Punna Reddy (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST)) ;
  • Ku, Su-Jin (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST)) ;
  • Choi, Yeon-Hee (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST)) ;
  • Park, Ji-Yeon (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST)) ;
  • Han, So-Yeop (Department of Chemistry and Nano Science, Ewha Womans University) ;
  • Baek, Du-Jong (Department of Chemistry, College of Natural Sciences, Sangmyung University) ;
  • Lee, Jae-Kyun (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST)) ;
  • Pae, Ae-Nim (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST)) ;
  • Min, Sun-Joon (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST)) ;
  • Cho, Yong-Seo (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
  • Received : 2011.04.07
  • Accepted : 2011.05.26
  • Published : 2011.08.20
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Abstract

The synthesis and biological evaluation of 1-heteroarylmethyl 1,4-diazepane derivatives as potential T-type calcium channel blockers is described. In this study, we have identified the compound 21i exhibiting the most potent T-type calcium channel blocking activity with $IC_{50}$ value of 0.20 ${\mu}M$, which is superior to that of mibefradil.

Keywords

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