Solution and solid-supported synthesis of 3,4,5-trisubstituted 1,2,4-triazole-based peptidomimetics |
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| Authors: | Boeglin Damien Cantel Sonia Heitz Annie Martinez Jean Fehrentz Jean-Alain |
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| Affiliation: | Laboratoire des Aminoacides, Peptides et Protéines (LAPP), UMR 5810 CNRS, Universités Montpellier I et II, Faculté de Pharmacie, 15 Avenue Charles Flahault, BP 14491, 34093 Montpellier Cédex 5, France. |
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| Abstract: | [reaction: see text] 3,4,5-Trisubstituted 1,2,4-triazoles were synthesized in solution from various thioamides and hydrazides in smooth experimental conditions leading to peptidomimetic scaffolds. This strategy was found to be compatible with the usual peptide synthesis protecting groups. This methodology was then applied on solid support by anchoring alpha-amino acids through their amino function to an activated carbonate resin. |
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