Atrial fibrillation is the most prevalent form of cardiac arrhythmia. Current treatments extend the atrial effective refractory period by nonselective blockade of cardiac ion channels. An alternative approach selectively targeting the Kv1.5 ion channel offers the opportunity for therapeutic benefit with decreased risk of adverse cardiovascular events. KVI-020 (4g) successfully demonstrated antiarrhythmic efficacy in a canine arrhythmia model, and these findings support its utility as an antiarrhythmic agent.

Download full-text PDF

Source
http://dx.doi.org/10.1021/jm901042mDOI Listing

Publication Analysis

Top Keywords

selective kv15
4
kv15 blockers
4
blockers development
4
development r-1-methylsulfonylamino-3-[2-4-methoxyphenylethyl]-4-4-methoxyphenyl-2-imidazolidinone
4
r-1-methylsulfonylamino-3-[2-4-methoxyphenylethyl]-4-4-methoxyphenyl-2-imidazolidinone kvi-020/wye-160020
4
kvi-020/wye-160020 potential
4
potential treatment
4
treatment atrial
4
atrial arrhythmia
4
arrhythmia atrial
4

Similar Publications

Pseudosaccharin amines as potent and selective KV1.5 blockers.

Bioorg Med Chem Lett

November 2015

Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.

Phenethyl aminoheterocycles like compound 1 were known to be potent I(Kur) blockers although they lacked potency in vivo. Modification of the heterocycle led to the design and synthesis of pseudosaccharin amines. Compounds such as 14, 17d and 21c were found to be potent K(V)1.

View Article and Find Full Text PDF

Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors.

Bioorg Med Chem Lett

July 2014

Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08534-5400, USA.

Phenethylaminoheterocycles have been prepared and assayed for inhibition of the Kv1.5 potassium ion channel as a potential approach to the treatment of atrial fibrillation. A diverse set of heterocycles were identified as potent Kv1.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!