The design and synthesis of 4-alkynyl pyrazole derivatives has led to the identification of new class of PDE4 inhibitors. All these compounds were accessed for the first time via a facile Pd/C-CuI-PPh(3) mediated C-C bond forming reaction between an appropriate pyrazole iodide and various terminal alkynes. In vitro PDE4B inhibitory properties and molecular modeling studies of some of the compounds synthesized indicated that 4-alkynyl pyrazole could be a promising template for the discovery of novel PDE4 inhibitors.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2012.02.008 | DOI Listing |
Publication Analysis
Top Keywords
design synthesis
8
synthesis 4-alkynyl
8
4-alkynyl pyrazole
8
pde4 inhibitors
8
4-alkynyl pyrazoles
4
pyrazoles inhibitors
4
inhibitors pde4
4
pde4 practical
4
practical access
4
access pd/c-cu
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!