An efficient and straightforward approach toward enzymatic synthesis of secondary amides of peptides was developed. A number of peptide derivatives containing amide moiety at C-terminus was obtained via subtilisin catalysis in good yields under mild conditions. Biological activity of some peptamides is evaluated.
An efficient and straightforward proteolytic enzyme-catalyzed approach towards the regioselective synthesis of nucleopeptides was developed. Appropriate reaction conditions were investigated and certain peptide-modified nucleosides were obtained with 70–90% yields. The obtained compounds could be efficiently used for medicinal diagnostic kits and therapeutic treatment.
Two ways for semi-enzymatic preparation of the peptide aldehydes are proposed: (1) enzymatic acylation of amino alcohols with acyl peptide esters and subsequent chemical oxidation of the resulting peptide alcohols with DMSO/acetic anhydride mixture or (2) enzymatic acylation of the preliminarily obtained by a chemical route amino aldehyde semicarbazones. Subtilisin 72, serine proteinase with a broad...
An enzymatic synthesis of peptidyl amino alcohols is described. The reactions were performed in organic solvents using as a catalyst subtilisin distributed on the surface of macroporous silica. Subsequent mild oxidation of peptidyl amino alcohols results in peptide aldehydes - the potent specific inhibitors of serine proteinases.
An enzymatic synthesis of Ac-Tyr-Ile-Gly-Ser-Arg-OH, its amide and p-nitroanilide starting with Boc-Ile-Gly-Ser-OCH 3 is described. The reactions were performed in organic solvents using subtilisin and α-chymotrypsin sorbed on macroporous silica surface as the catalysts.
p-Nitroanilides of N-acylated di-, tri- and tetrapeptides with C-terminal arginine or lysine residues have been obtained, as a rule with good yields, via acylation of arginine or lysine p-nitroanilides by methyl esters of respective N-acylated peptides, catalyzed by subtilisin or α-chymotrypsin. The synthesis might be performed by two routes--by reaction in water-organic solvent mixtures, catalyzed...
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