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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Use of Click-Chemistry in the Development of Peptidomimetic Enzyme Inhibitors

Author(s): P. Fabbrizzi, G. Menchi, A. Guarna and A. Trabocchi

Volume 21 , Issue 13 , 2014

Page: [1467 - 1477] Pages: 11

DOI: 10.2174/0929867321666131218093611

Price: $65


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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