Backbone-Fluorinated 1,2,3-Triazole-Containing Dipeptide Surrogates
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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.
Originalsprog | Engelsk |
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Tidsskrift | Journal of Organic Chemistry |
Vol/bind | 82 |
Udgave nummer | 21 |
Sider (fra-til) | 11613-11619 |
ISSN | 0022-3263 |
DOI | |
Status | Udgivet - 16 okt. 2017 |
ID: 184573364