756485-04-8Relevant academic research and scientific papers
PROCESS FOR PRODUCING PEPTIDYL ALDEHYDES
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, (2008/06/13)
The present invention provides a method of producing a peptidyl aldehyde derivative of the formula (II) wherein A is acyl derived from amino acid, and R1 and R2 are different and one is hydrogen atom and the other is optionally subst
Inhibitors of β-amyloid protein production
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, (2008/06/13)
This invention relates to compounds and pharmaceutical compositions, and methods for inhibiting or preventing the amyloid protein deposits in the brain which are associated with Alzheimer's disease and aged Down's syndrome patients. More particularly, it relates to the treatment of Alzheimer's disease.
Solid Phase Synthesis of C-Terminal Peptide Aldehydes
Fehrentz,Paris,Heitz,Velek,Winternitz,Martinez
, p. 6792 - 6796 (2007/10/03)
Peptides with C-terminal aldehydes (PAs) are of interest due to their inhibitory properties toward numerous classes of proteolytic enzymes. In this paper, we describe and compare two novel approaches for the preparation of PAs by solid phase synthesis, on
Use of ozonolysis in the synthesis of C-terminal peptide aldehydes on solid support
Pothion, Catherine,Paris, Marielle,Heitz, Annie,Rocheblave, Luc,Rouch, Florence,Fehrentz, Jean-Alain,Martinez, Jean
, p. 7749 - 7752 (2007/10/03)
A new strategy for the synthesis of peptide aldehydes on solid support is presented. Reaction of a N-protected aminoaldehyde with caboethoxymethylene triphenylphosphorane yielded an α-β-unsaturated δ- amino derivative. After saponification, the resulting α-β-unsaturated δ- aminoacid was anchored to a solid support by an ester linkage (Merrifield resin) or by an amide linkage (MBHA, Expansin). After elongation of the peptide chain, ozonolysis yielded quite pure C-terminal peptide aldehydes in a good yield with no detectable racemization of the C-terminal residue.
Vanadium(II)- and Niobium(III)-Induced, Diastereoselective Pinacol Coupling of Peptide Aldehydes to Give a C2-Symmetrical HIV Protease Inhibitor
Kammermeier, Bernhard,Beck, Gerhard,Holla, Wolfgang,Jacobi, Detlev,Napierski, Bernd,Jendralla, Heiner
, p. 307 - 315 (2007/10/03)
Peptide aldehydes 15a-c are prepared without epimerization from enantiomerically pure (S)-α-amino acids (Scheme 3).Reductive pinacol homocoupling of 15a-c, induced by vanadium complex 11 or niobium complex 16 in refluxing THF, yields C2-symmetr
Improved solid phase synthesis of C-terminal peptide aldehydes
Fehrentz, Jean-Alain,Paris, Marielle,Heitz, Annie,Velek, Jiri,Liu, Chuan-Fa,et al.
, p. 7871 - 7874 (2007/10/02)
A new linker based on the Weinreb amide was developed in order to synthesize from peptidyl-resin the corresponding aldehydic peptides by reduction with LiAlH4.This new reaction was tested with N-protected amino-residues and with tripeptides to obtain the
Inhibitors of HIV-1 proteinase containing 2-heterosubstituted 4-amino-3- hydroxy-5-phenylpentanoic acid: Synthesis, enzyme inhibition, and antiviral activity
Scholz,Billich,Charpiot,Ettmayer,Lehr,Rosenwirth,Schreiner,Gstach
, p. 3079 - 3089 (2007/10/02)
A convenient procedure for the synthesis of 2-heterosubstituted statine derivatives as novel building blocks in HIV-protease inhibitors has been developed. The synthesis starts with protected L-phenylalaninols, which were converted to γ-amino α,β-unsatura
