PHOSPHORUS-ACID ANALOGS OF L-680,833, A POTENT MONOCYCLIC BETA-LACTAMINHIBITOR OF HUMAN-LEUKOCYTE ELASTASE

Authors
DURETTE PL CHABIN RM FLETCHER DS GREEN BG HANLON WA HUMES JL KNIGHT WB LANZA TJ MUMFORD RA PACHOLOK S MACCOSS M
Citation
Pl. Durette et al., PHOSPHORUS-ACID ANALOGS OF L-680,833, A POTENT MONOCYCLIC BETA-LACTAMINHIBITOR OF HUMAN-LEUKOCYTE ELASTASE, Bioorganic & medicinal chemistry letters, 5(3), 1995, pp. 271-274
Citations number
6
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
3
Year of publication
1995
Pages
271 - 274
Database
ISI
SICI code
0960-894X(1995)5:3<271:PAOLAP>2.0.ZU;2-6
Abstract
Analogs of the monocyclic beta-lactam human leukocyte elastase (HLE) i nhibitor L-680,833 in which the carboxyl group is replaced by phosphor ous acid moieties were synthesized and found to be potent inhibitors o f the enzyme (k(inact)/K-i in the range 217,000-1,326,000 M(-1)s(-1)). Cellular activity was demonstrated by inhibition of the generation of the N-terminal cleavage product A alpha-(1-21) from the A alpha chain of fibrinogen.