We report here the total synthesis of B-973 (five steps), a recently identified α7 nAChR ago-PAM, its enantiomeric resolution, and its electrophysiological characterization in oocytes to identify (-)-B-973B as the bioactive enantiomer. The asymmetric synthesis of B-973B was accomplished in 99% ee, and X-ray crystallography studies revealed its absolute "" stereochemistry. B-973B was effective in attenuating pain behavior and decreasing paw edema (formalin test), and its analgesic effects were mediated through α7 nAChR.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6231182 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.8b00407 | DOI Listing |
Publication Analysis
Top Keywords
α7 nachr
12
nachr ago-pam
8
asymmetric synthesis
8
b-973 novel
4
novel α7
4
ago-pam racemic
4
racemic asymmetric
4
synthesis electrophysiological
4
electrophysiological studies
4
studies evaluation
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!