Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers |
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| Authors: | Su Jin Gu Jae Kyun Lee Ae Nim Pae Hye Jin Chung Hyewon Rhim So Yeob Han Sun-Joon Min Yong Seo Cho |
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| Institution: | 1. Life/Health Division, Korea Institute of Science and Technology, PO Box 131, Cheongyang, Seoul 130-650, Republic of Korea;2. Department of Chemistry and Nano Science, Ewha Womans University, Seoul 130-701, Republic of Korea |
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| 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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