Copper catalyzed azide-alkyne cycloaddition (CuAAC) chemistry is reported for the construction of previously unknown 5-(1H-1,2,3-triazol-1-yl)-4,5'-bithiazoles from 2-bromo-1-(thiazol-5-yl)ethanones. These novel triazolobithiazoles are shown to have cystic fibrosis (CF) corrector activity and, compared to the benchmark bithiazole CF corrector corr-4a, improved logP values (4.5 vs 5.96).
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3419814 | PMC |
| http://dx.doi.org/10.1016/j.bmc.2012.06.046 | DOI Listing |
Publication Analysis
Top Keywords
cystic fibrosis
8
click-based synthesis
4
synthesis triazolobithiazole
4
triazolobithiazole Δf508-cftr
4
Δf508-cftr correctors
4
correctors cystic
4
fibrosis copper
4
copper catalyzed
4
catalyzed azide-alkyne
4
azide-alkyne cycloaddition
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!