The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K

[Image: see text] Irreversible covalent inhibitors can have a beneficial pharmacokinetic/pharmacodynamics profile but are still often avoided due to the risk of indiscriminate covalent reactivity and the resulting adverse effects. To overcome this potential liability, we introduced an alkyne moiety...

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Detalhes bibliográficos
Publicado no:J Am Chem Soc
Main Authors: Mons, Elma, Jansen, Ineke D. C., Loboda, Jure, van Doodewaerd, Bjorn R., Hermans, Jill, Verdoes, Martijn, van Boeckel, Constant A. A., van Veelen, Peter A., Turk, Boris, Turk, Dusan, Ovaa, Huib
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2019
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6396318/
https://ncbi.nlm.nih.gov/pubmed/30689386
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jacs.8b11027
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