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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 32, Number 8
BKCSDE 32(8)
August 20, 2011 

Synthesis and Biological Evaluation of 1-Heteroarylmethyl 1,4-Diazepanes Derivatives as Potential T-type Calcium Channel Blockers
Punna Reddy Ullapu, Su Jin Ku, Yeon Hee Choi,¶ Jiyeon Park,¶ So-Yeop Han, Du Jong Baek,¶ Jaekyun Lee, Ae Nim Pae, Sun-Joon Min,*, Yong Seo Cho,*,
T-type calcium channel blockers, 1,4-Diazepanes, Heteroaromatic compounds, FDSS6000 assay, Patch-clamp assay
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 IC50 value of 0.20 μM, which is superior to that of mibefradil.
3063 - 3073
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