INHIBITION OF HUMAN-LEUKOCYTE ELASTASE .7. INHIBITION BY 6-SUBSTITUTED PENICILLIN AMIDES

Authors
THOMPSON KR FINKE PE SHAH SK ASHE BM DAHLGREN ME DELLEA PS FLETCHER DS HAND KM MAYCOCK AL DOHERTY JB
Citation
Kr. Thompson et al., INHIBITION OF HUMAN-LEUKOCYTE ELASTASE .7. INHIBITION BY 6-SUBSTITUTED PENICILLIN AMIDES, Bioorganic & medicinal chemistry letters, 3(11), 1993, pp. 2289-2294
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
3
Issue
11
Year of publication
1993
Pages
2289 - 2294
Database
ISI
SICI code
0960-894X(1993)3:11<2289:IOHE.I>2.0.ZU;2-F
Abstract
Penicillin amides substituted at C-6 with either an alpha- or beta-tri fluoroacetamido or an alpha-alkoxy functionality are reported as human leukocyte elastase (HLE) inhibitors. The structure activity relations for these derivatives are discussed and compared to the corresponding known cephalosporin structures in terms of chemical stability, HLE in hibition, and efficacy in an intratracheal (IT) lung hemorrhage assay.