Backbone-Fluorinated 1,2,3-Triazole-Containing Dipeptide Surrogates
Research output: Contribution to journal › Journal article › Research › peer-review
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.
Original language | English |
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Journal | Journal of Organic Chemistry |
Volume | 82 |
Issue number | 21 |
Pages (from-to) | 11613-11619 |
ISSN | 0022-3263 |
DOIs | |
Publication status | Published - 16 Oct 2017 |
- Journal Article
Research areas
ID: 184573364