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Backbone-Fluorinated 1,2,3-Triazole-Containing Dipeptide Surrogates

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Jens Engel-Andreasen, Isabelle Wellhöfer, Kathrine Wich, Christian A Olsen

The 1,2,3-triazole moiety can be incorporated as a peptide bond bioisostere to provide protease resistance in peptidomimetics. Herein, we report the synthesis of peptidomimetic building blocks containing backbone-fluorinated 1,4-disubstituted 1,2,3-triazole moieties. Synthetic protocols for the preparation of various Xaa-Gly dipeptide surrogates in the form of Xaa-ψ[triazole]-F2Gly building blocks were established, and selected examples were introduced into the endogenous peptide opioid receptor ligand Leu-enkephalin as a model compound.

OriginalsprogEngelsk
TidsskriftJournal of Organic Chemistry
Vol/bind82
Tidsskriftsnummer21
Sider (fra-til)11613-11619
ISSN0022-3263
DOI
StatusUdgivet - 16 okt. 2017

ID: 184573364