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.
Keywords: Cycloaddition, drug discovery, enzymes, high-throughput screening, organic synthesis.
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