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Št. zadetkov: 3
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)
Incorporation of the trifluoromethylthio group (CF [sub] 3S−) into biomolecules
Jure Gregorc, Nathalie Lensen, Grégory Chaume, Jernej Iskra, Thierry Brigaud
Pregledni znanstveni članek
Oznake: fluor;biomolekule;peptidi;aminokisline;NMR spektroskopija;farmakokinetika;fluorine;biomolecules;peptides;amino acids;NMR spectroscopy;pharmacokinetics;
The trifluoromethylthio functional group (CF$_3$S-) has gained considerable attention in synthetic and medicinal chemistry due to its ability to enhance the pharmacokinetic profiles of functionalized compounds. This Synopsis highlights recent progress in the incorporation of the CF$_3$S group into b ...
Leto: 2026 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: 3
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