SYNTHESIS OF CEPHALOSPORIN OLIGOPEPTIDES AS POTENTIAL PROTEINASE-INHIBITORS

Authors
PITLIK J BAGOSSI P JEKO J TOZSER J
Citation
J. Pitlik et al., SYNTHESIS OF CEPHALOSPORIN OLIGOPEPTIDES AS POTENTIAL PROTEINASE-INHIBITORS, Die Pharmazie, 51(10), 1996, pp. 700-704
Citations number
35
Categorie Soggetti
Pharmacology & Pharmacy",Chemistry
Journal title
Die Pharmazie → ACNP
ISSN journal
00317144
Volume
51
Issue
10
Year of publication
1996
Pages
700 - 704
Database
ISI
SICI code
0031-7144(1996)51:10<700:SOCOAP>2.0.ZU;2-U
Abstract
Synthesis of cephalosporin oligopeptides from 7 beta-amino-desacetoxyc ephalosporanic acid and hydrophobic amino acids is described. Their in vitro inhibitory activities against porcine pancreatic elastase, alph a-chymotrypsin and human immunodeficiency virus type 1 proteinase (HIV -1 PR) were tested by spectroscopic assays and against HIV-1 PR also b y a HPLC assay. Up to 0.2 mM concentration they did not show any inhib ition. However, using the HPLC method, they were found to be weak inhi bitors of HIV-1 PR, with IC50 values in the millimolar range.