We identified and characterized a series of pyrrole amides as potent, selective Ca3.2-blockers. This series culminated with the identification of pyrrole amides 13b and 26d, with excellent potencies and/or selectivities toward the Ca3.1- and Ca3.3-channels. These compounds display poor physicochemical and DMPK properties, making their use difficult for in vivo applications. Nevertheless, they are well-suited for in vitro studies.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2017.09.062 | DOI Listing |
Publication Analysis
Top Keywords
pyrrole amides
8
discovery evaluation
4
evaluation ca32-selective
4
ca32-selective t-type
4
t-type calcium
4
calcium channel
4
channel blockers
4
blockers identified
4
identified characterized
4
characterized series
4
Similar Publications
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!