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Št. zadetkov: 2
Trifluoromethylthiolation of tryptophan and tyrosine derivatives
Jure Gregorc, Nathalie Lensen, Grégory Chaume, Jernej Iskra, Thierry Brigaud
Izvirni znanstveni članek
Oznake: aromatske spojine;hidrofobnost;monomeri;peptidi;proteini;reakcijski produkti;aromatic compounds;hydrophobicity;monomers;peptides;proteins;reaction products;
The incorporation of fluorinated groups into peptides significantly affects their biophysical properties. We report herein the synthesis of Fmoc-protected trifluoromethylthiolated tyrosine (CF$_3$S-Tyr) and tryptophan (CF$_3$S-Trp) analogues on a gram scale (77–93% yield) and demonstrate their use a ...
Leto: 2023 Vir: Fakulteta za kemijo in kemijsko tehnologijo (UL FKKT)
Trifluoromethylthio and trifluoromethyl functionalization of endomorphin-1 enhances its hydrophobicity and plasma stability while preserving its affinity for the [mu]-opioid receptor
Jure Gregorc, Jolien De Neve, Karine Guitot, Brian J. Holleran, Nathalie Lensen, Louis Gendron, Thierry Brigaud, Jernej Iskra, Steven Ballet, Grégory Chaume
Izvirni znanstveni članek
Oznake: ligandi;peptidi;opioidni receptorji;fluor;metabolna stabilnost;ligands;peptides;opioid receptors;fluorine;metabolic stability;
The incorporation of fluorinated amino acid residues into peptides represents a promising strategy for improving the pharmacokinetic properties of bioactive peptides. Herein, we report the solid-phase synthesis (SPPS) of a set of ten SCF$_{3^-}$ or CF$_{3^-}$ modified neuropeptide analogs based on e ...
Leto: 2026 Vir: Fakulteta za kemijo in kemijsko tehnologijo (UL FKKT)
Št. zadetkov: 2
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