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New methods for solid phase peptide synthesis of transitionstate analog inhibitors of HIV-1 protease and DPP-IV

par Piron, Jan;Tourwe, Dirk
Référence Letters in Peptide Science, 2, 3-4, page (229-232)
Publication Publié, 1995-11

Article révisé par les pairs

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Résumé :

A new and stereoselective method to synthesize hydroxyethylamine and hydroxymethylamide peptide bond isosteres is developed. The key step is the addition of 2-trimethylsilylthiazole to α-aminoaldehydes, followed by transformation to α-hydroxy-β-aminoaldehydes. The stereochemistry of the addition can be manipulated by the choice of the nitrogen substitution. The isosteres are easily synthesized via Solid Phase Peptide Synthesis, which rapidly gives the desired pseudopeptides. © 1995 ESCOM Science Publishers B.V.