THE SYNTHESIS AND SERINE BETA-LACTAMASE INHIBITORY ACTIVITY OF SOME PHOSPHONAMIDATE ANALOGS OF DIPEPTIDES

Authors
BATESON JH GASSON BC KHUSHI T NEALE JE PAYNE DJ TOLSON DA WALKER G
Citation
Jh. Bateson et al., THE SYNTHESIS AND SERINE BETA-LACTAMASE INHIBITORY ACTIVITY OF SOME PHOSPHONAMIDATE ANALOGS OF DIPEPTIDES, Bioorganic & medicinal chemistry letters, 4(14), 1994, pp. 1667-1672
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
14
Year of publication
1994
Pages
1667 - 1672
Database
ISI
SICI code
0960-894X(1994)4:14<1667:TSASBI>2.0.ZU;2-F
Abstract
The dipeptidyl phosphonamidate analogues (4)-(12) inhibited a range of serine beta-lactamases, being most efficacious against the Enterobact er cloacae P99 isolated enzyme. Synergy experiments demonstrated that the antibacterial activity of amoxycillin is potentiated against bacte ria producing these enzymes, the effect again being most pronounced ag ainst the P99-producing E.cloacae N-1 strain. The analogues (11) and ( 12) (beta-amino acid C-terminal) were the most active inhibitors and s ynergists.