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

P.      Fabbrizzi; G.      Menchi; A.      Guarna; A.      Trabocchi

Abstract

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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Current Medicinal Chemistry

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

Volume: 21 Issue: 13

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

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

Abstract: 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.

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Fabbrizzi P., Menchi G., Guarna A. and Trabocchi A., Use of Click-Chemistry in the Development of Peptidomimetic Enzyme Inhibitors , Current Medicinal Chemistry 2014; 21 (13) . https://dx.doi.org/10.2174/0929867321666131218093611

DOI https://dx.doi.org/10.2174/0929867321666131218093611	Print ISSN 0929-8673
Publisher Name Bentham Science Publisher	Online ISSN 1875-533X

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