The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate

  • Bioorg Med Chem Lett. 2001 Apr 9;11(7):895-8. doi: 10.1016/s0960-894x(01)00078-6.
S J Macdonald  1 ,  M D Dowle ,  L A Harrison ,  P Shah ,  M R Johnson ,  G G Inglis ,  G D Clarke ,  R A Smith ,  D Humphreys ,  C R Molloy ,  A Amour ,  M Dixon ,  G Murkitt ,  R E Godward ,  T Padfield ,  T Skarzynski ,  O M Singh ,  K A Kumar ,  G Fleetwood ,  S T Hodgson ,  G W Hardy ,  H Finch
Affiliations
  • 1. Medicinal Chemistry 2, GlaxoWellcome Medicines Research Centre, Stevenage, UK. [email protected]
PMID: 11294386 DOI: 10.1016/s0960-894x(01)00078-6
Abstract

The discovery of a potent intracellular inhibitor of human neutrophil Elastase which is orally active and has a long duration of action is described. The pharmacodynamic and pharmacokinetic properties of a trans-lactam development candidate, GW311616A, are described.

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