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

Autor: Macdonald, Simon J.F, Dowle, Michael D, Harrison, Lee A, Shah, Pritom, Johnson, Martin R, Inglis, Graham G.A, Clarke, Geoffrey D.E, Smith, Robin A, Humphreys, Davina, Molloy, Christopher R, Amour, Augustin, Dixon, Mary, Murkitt, Graham, Godward, Rosalind E, Padfield, Tony, Skarzynski, Tadeusz, Singh, Onkar M.P, Kumar, K.Abhhilash, Fleetwood, Gill, Hodgson, Simon T, Hardy, George W, Finch, Harry

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 2001 11(7):895-898

Corrigendum to “Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine- trans-lactams” : [Bioorg. Med. Chem. Lett. 11 (2001) 243]

Autor: Macdonald, Simon J.F., Dowle, Michael D., Harrison, Lee A., Spooner, Julie E., Shah, Pritom, Johnson, Martin R., Inglis, Graham G.A., Clarke, Geoffrey D.E., Belton, David J., Smith, Robin A., Molloy, Christopher R., Dixon, Mary, Murkitt, Graham, Godward, Rosalind E., Skarzynski, Tadeusz, Singh, Onkar M.P., Kumar, K.Abhhilash, Hodgson, Simon T., McDonald, Edward, Hardy, George W., Finch, Harry, Humphreys, Davina C., Fleetwood, Gill

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 2001 11(9):1249-1249

Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).

Autor: Macdonald SJ; Medicinal Chemistry 1, In Vitro Pharmacology, Systems Research, Respiratory Systems, Stevenage CEDD DMPK, United Kingdom. sjfm5947@gsk.com, Dowle MD, Harrison LA, Clarke GD, Inglis GG, Johnson MR, Shah P, Smith RA, Amour A, Fleetwood G, Humphreys DC, Molloy CR, Dixon M, Godward RE, Wonacott AJ, Singh OM, Hodgson ST, Hardy GW

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2002 Aug 29; Vol. 45 (18), pp. 3878-90.