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THE GROWING IMPACT OF CLICK CHEMISTRY ON DRUG DISCOVERY

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The growing impact of click chemistry on drug discovery

HC Kolb, KB SharplessDrug discovery today, 2003 – Elsevier

Click chemistry is a modular approach that uses only the most practical and reliable
chemical transformations. Its applications are increasingly found in all aspects of drug
discovery, ranging from lead finding through combinatorial chemistry and target-templated
 
Click chemistry is a modular approach that uses only the most practical
and reliable chemical transformations. Its applications are increasingly
found in all aspects of drug discovery, ranging from lead finding through
combinatorial chemistry and target-templated in situchemistry, to proteomics
and DNA research, using bioconjugation reactions. The copper-(I)-catalyzed
1,2,3-triazole formation from azides and terminal acetylenes is a particularly
powerful linking reaction, due to its high degree of dependability, complete
specificity, and the bio-compatibility of the reactants. The triazole products
are more than just passive linkers; they readily associate with biological
targets, through hydrogen bonding and dipole interactions.
 
 
 

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Filed under: Drug discovery Tagged: CLICK CHEMISTRY, drug discovery

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