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

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 pharmacok...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-05, Vol.20 (9), p.2705-2708
Main Authors: Gu, Su Jin, Lee, Jae Kyun, Pae, Ae Nim, Chung, Hye Jin, Rhim, Hyewon, Han, So Yeob, Min, Sun-Joon, Cho, Yong Seo
Format: Article
Language:English
Subjects:
1,4-Diazepane
Administration, Oral
Animals
Antihypertensive Agents - chemical synthesis
Antihypertensive Agents - chemistry
Antihypertensive Agents - pharmacokinetics
Azepines - chemical synthesis
Azepines - chemistry
Azepines - pharmacokinetics
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacokinetics
Biological and medical sciences
Calcium Channel Blockers - chemical synthesis
Calcium Channel Blockers - chemistry
Calcium Channel Blockers - pharmacokinetics
Calcium Channels, T-Type - chemistry
Calcium Channels, T-Type - metabolism
Cardiovascular system
Cell Line
Humans
Medical sciences
Miscellaneous
Pharmacokinetics
Pharmacology. Drug treatments
Rats
T-type calcium channel blockers
Trans-Activators - metabolism
Transcriptional Regulator ERG
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Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.03.084