P. Fabbrizzi, G. Menchi, A. Guarna and A. Trabocchi Pages 1467 - 1477 ( 11 )
Cu(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) is often utilized in medicinal chemistry to make the triazole moiety as it acts as a non-classical bioisostere of the peptide bond. This useful technique can also be applied in the fragment-based assembly of molecular libraries for high-throughput screening. This minireview outlines the application of click-chemistry in the synthesis of enzyme inhibitors with the triazole moiety.
Cycloaddition, drug discovery, enzymes, high-throughput screening, organic synthesis.
, , , Department of Chemistry "Ugo Schiff" , University of Florence, via della Lastruccia 13, I-50019 Sesto Fiorentino, Florence, Italy.