dipeptidyl hydroxamic acids (H-X-Gly-NHOH: X = amino acid residues) was synthesized, and the inhibitory activity against Jackbean and Proteus mirabilis ureases [EC3.5.1.5] was examined. A number of H-X-Gly-NHOH inhibited Jackbeanurease with an I50 of the order of 10(-6) M and inhibited Proteus mirabilis urease with an I50 of the order of 10(-5) M. The inhibition against Jackbeanurease was more potent
replacement of the N-benzyloxycarbonyl (Z) group in the Anderson peptide (Z–Gly–L/D–Phe–Gly–OEt) by Z–L-Ala and the subsequent separation of the diastereomers of the resulting tetrapeptide by reversed-phase HPLC offer a more convenient version with higher accuracy to the original Anderson test for studying racemization in peptidesynthesis.
Thiopeptolide substrates for vertebrate collagenase
申请人:Monsanto Company
公开号:US04569907A1
公开(公告)日:1986-02-11
The disclosure relates to novel synthetic thiopeptolide substrates having high activity for the enzyme collagenase. These substrates have the following amino acid sequences: R-Pro-X-Gly-S-Y-Z-Gly-R.sub.1 wherein R=H or N-protecting group, X=Leu, Ile, Phe, Val, Gln, Ala, Y=Leu, Ile, Phe, Val, Ala, Z=Leu, Ile, Phe, Val, Gln, Ala, and R.sub.1 =terminal amide, carboxyl or ester group.
Novel thiopeptolide substrates for vertebrate collagenase
申请人:Monsanto Company
公开号:US04596675A1
公开(公告)日:1986-06-24
The disclosure relates to novel synthetic thiopeptolide substrates having high activity for the enzyme collagenase. These substrates have the following amino acid sequences: R-Pro-X-Gly-S-Y-Z-Gly-R.sub.1 wherein R=H or N-protecting group, X=Leu, Ile, Phe, Val, Gln, Ala, Y=Leu, Ile, Phe, Val, Ala, Z=Leu, Ile, Phe, Val, Gln, Ala, and R.sub.1 =terminal amide, carboxyl or ester group.
Synthesis and characterization by 13C-CP-MAS- and high resolution 1H-, 13C-NMR of new ureido sugars, derivatives of methyl 2-amino-2-deoxy-β-d-glucopyranose and dipeptides
Dipeptide ethyl and benzyl esters were used as amination agents in reaction with methyl 3,4,6-tri-O-acetyl-2-deoxy-2-(4-nitrophenoxycarbonylamino)-beta-D-glucopyranoside(1). Ten new ureido sugars, derivatives of GlyAla, AlaGly, AlaAla, GlyVal, ValGly, LeuGly, PheGly, GlyPhe, and AlaPhe; were obtained. The new ureido sugars were studied by means of H-1- and C-13-NMR spectroscopy in solution, and C-13-CP-MAS-NMR in the solid-state. (C) 1997 Elsevier Science Ltd. All rights reserved.