Synthesis of cephalosporin oligopeptides as potential proteinase inhibitors

Research output: Article

7 Citations (Scopus)

Abstract

Synthesis of cephalosporin oligopeptides from 7β-amino-desacetoxycephalosporanic acid and hydrophobic amino acids is described. Their in vitro inhibitory activities against porcine pancreatic elastase, α-chymotrypsin and human immunodeficiency virus type 1 proteinase (HIV-1 PR) were tested by spectroscopic assays and against HIV-1 PR also by a HPLC assay. Up to 0.2 mM concentration they did not show any inhibition. However, using the HPLC method, they were found to be weak inhibitors of HIV-1 PR, with IC50 values in the millimolar range.

Original languageEnglish
Pages (from-to)700-704
Number of pages5
JournalPharmazie
Volume51
Issue number10
Publication statusPublished - okt. 1996

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Oligopeptides
Cephalosporins
Viruses
HIV-1
Peptide Hydrolases
Assays
High Pressure Liquid Chromatography
Amino Acids
Pancreatic Elastase
Chymotrypsin
Inhibitory Concentration 50
Amino acids
Swine

ASJC Scopus subject areas

  • Molecular Medicine
  • Chemistry(all)
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science
  • Pharmacology

Cite this

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abstract = "Synthesis of cephalosporin oligopeptides from 7β-amino-desacetoxycephalosporanic acid and hydrophobic amino acids is described. Their in vitro inhibitory activities against porcine pancreatic elastase, α-chymotrypsin and human immunodeficiency virus type 1 proteinase (HIV-1 PR) were tested by spectroscopic assays and against HIV-1 PR also by a HPLC assay. Up to 0.2 mM concentration they did not show any inhibition. However, using the HPLC method, they were found to be weak inhibitors of HIV-1 PR, with IC50 values in the millimolar range.",
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AU - Bagossi, P.

AU - Jekó́, J.

AU - Tőzsér, J.

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N2 - Synthesis of cephalosporin oligopeptides from 7β-amino-desacetoxycephalosporanic acid and hydrophobic amino acids is described. Their in vitro inhibitory activities against porcine pancreatic elastase, α-chymotrypsin and human immunodeficiency virus type 1 proteinase (HIV-1 PR) were tested by spectroscopic assays and against HIV-1 PR also by a HPLC assay. Up to 0.2 mM concentration they did not show any inhibition. However, using the HPLC method, they were found to be weak inhibitors of HIV-1 PR, with IC50 values in the millimolar range.

AB - Synthesis of cephalosporin oligopeptides from 7β-amino-desacetoxycephalosporanic acid and hydrophobic amino acids is described. Their in vitro inhibitory activities against porcine pancreatic elastase, α-chymotrypsin and human immunodeficiency virus type 1 proteinase (HIV-1 PR) were tested by spectroscopic assays and against HIV-1 PR also by a HPLC assay. Up to 0.2 mM concentration they did not show any inhibition. However, using the HPLC method, they were found to be weak inhibitors of HIV-1 PR, with IC50 values in the millimolar range.

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