Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors

Jürgen Seibel; David Brown; Augustin Amour; Simon J Macdonald; Neil J Oldham; Christopher J Schofield

doi:10.1016/s0960-894x(02)00995-2

Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors

Bioorg Med Chem Lett. 2003 Feb 10;13(3):387-9. doi: 10.1016/s0960-894x(02)00995-2.

Authors

Jürgen Seibel¹, David Brown, Augustin Amour, Simon J Macdonald, Neil J Oldham, Christopher J Schofield

Affiliation

¹ The Oxford Centre for Molecular Sciences and The Dyson Perrins Laboratory, South Parks Road, Oxford OX1 3QY, UK.

PMID: 12565935
DOI: 10.1016/s0960-894x(02)00995-2

Abstract

A series of monocyclic delta-lactams (piperazones) was prepared and analysed as inhibitors of porcine pancreatic elastase and human neutrophil elastase.

MeSH terms

Animals
Cyclization
Humans
Indicators and Reagents
Kinetics
Lactams / chemical synthesis*
Lactams / pharmacology*
Magnetic Resonance Spectroscopy
Pancreatic Elastase / antagonists & inhibitors*
Serine Proteinase Inhibitors / chemical synthesis*
Serine Proteinase Inhibitors / pharmacology*
Spectrometry, Mass, Electrospray Ionization
Swine

Substances

Indicators and Reagents
Lactams
Serine Proteinase Inhibitors
Pancreatic Elastase