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2-Cyanoisonicotinamide Conjugation: A Facile Approach to Generate Potent Peptide Inhibitors of the Zika Virus Protease

Patil, Nitin; Quek, Jun-Ping; Schroeder, Barbara; Morewood, Richard; Rademann, Jörg; Luo, Dahai; Nitsche, Christoph


The rapid generation and modification of macrocyclic peptides in medicinal chemistry is an ever-growing area that can present various synthetic challenges. The reaction between N-terminal cysteine and 2-cyanoisonicotinamide is a new biocompatible click reaction that allows rapid access to macrocyclic peptides. Importantly, 2-cyanoisonicotinamide can be attached to different linkers directly during solid-phase peptide synthesis. The synthesis involves only commercially available precursors,...[Show more]

CollectionsANU Research Publications
Date published: 2021-05-13
Type: Journal article
Source: ACS medicinal chemistry letters
DOI: 10.1021/acsmedchemlett.0c00657
Access Rights: Open Access


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