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Bioorg Med Chem Lett. 2001 Jan 22;11(2):243-6.

Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.

Author information

1
Medical Chemistry 2, Glaxo Wellcome Medicines Research Centre, Stevenage, UK. sjfm5947@glaxowellcome.co.uk

Erratum in

  • Bioorg Med Chem Lett 2001 May 7;11(9):1249.

Abstract

Described are the acylation binding of trans-lactam 1 to porcine pancreatic elastase, the selection of the SO2Me activating group for the lactam N which also confers metabolic stability in hamster liver microsomes, the introduction of aqueous solubility through the piperidine salt 9, the in vivo oral activity of 9 and its bioavailability, and the introduction of 9 as an intracellular neutrophil elastase inhibitor.

PMID:
11206469
DOI:
10.1016/s0960-894x(00)00632-6
[Indexed for MEDLINE]

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