Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors

Authors
Clemente, A Domingos, A Grancho, AP Iley, J Moreira, R Neres, J Palma, N Santana, AB Valente, E
Citation
A. Clemente et al., Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors, BIOORG MED, 11(8), 2001, pp. 1065-1068
Citations number
22
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
8
Year of publication
2001
Pages
1065 - 1068
Database
ISI
SICI code
0960-894X(20010423)11:8<1065:DSASON>2.0.ZU;2-L
Abstract
A series of N-acyloxymethyl- and N-aminocarbonyloxymethyl derivatives of 2- azetidinones. 3, with different substituent patterns at the beta -lactam C- 3 and C-4 positions, were designed as potential mechanism-based inhibitors for human leukocyte elastase and found to exhibit inhibitory potency and se lectivity for the enzyme, (C) 2001 Elsevier Science Ltd. All rights reserve d.