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)

Journal of Medicinal Chemistry

Volumn 45, Issue 18, 2002, Pages 3878-3890

  Macdonald, Simon J F ^a   Dowle, Michael D ^a   Harrison, Lee A ^a   Clarke, Geoffrey D E ^a   Inglis, Graham G A ^a   Johnson, Martin R ^a   Shah, Pritom ^a   Smith, Robin A ^a   Amour, Augustin ^a   Fleetwood, Gill ^a   Humphreys, Davina C ^a   Molloy, Christopher R ^a   Dixon, Mary ^a   Godward, Rosalind E ^a   Wonacott, Alan J ^a   Singh, Onkar M P ^a   Hodgson, Simon T ^a   Hardy, George W ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

3 ISOPROPYL 1 METHANESULFONYL 4 (2 PYRROLIDIN 1 YLMETHYLOXAZOLE 4 CARBONYL)HEXAHYDROPYRROLO[3,2 B]PYRROL 2 ONE; 4 (5 CYCLOPROPYLAMINOMETHYLPYRAZINE 2 CARBONYL) 3 ISOPROPYL 1 METHANESULFONYLHEXAHYDROPYRROLO[3,2 B]PYRROL 2 ONE; 4 [1 (2,2 DIMETHYLPROPYL)AZETIDINE 3 CARBONYL] 3 ISOPROPYL 1 METHANESULFONYLHEXAHYDROPYRROLO[3,2 B]PYRROL 2 ONE; GW 311616A; GW 447631; GW 469002; GW 475151; LACTAM DERIVATIVE; LEUKOCYTE ELASTASE; LEUKOCYTE ELASTASE INHIBITOR; N [1 (1,3 BENZODIOXOL 5 YL)BUTYL] 3,3 DIETHYL 2 [4 [(4 METHYL 1 PIPERAZINYL)CARBONYL]PHENOXY] 4 OXO 1 AZETIDINECARBOXAMIDE; PANCREATIC ELASTASE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BLOOD; CHRONOBIOLOGY; COMPLEX FORMATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; CRYSTALLIZATION; DOG; DOSE TIME EFFECT RELATION; DRUG CLEARANCE; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; ENANTIOMER; ENZYME INHIBITION; FEMALE; HAMSTER; HUMAN; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; PHARMACODYNAMICS; RAT; SPECIES DIFFERENCE; STRUCTURE ANALYSIS; SWINE; TRANS ISOMER;

ANIMALS; COMBINATORIAL CHEMISTRY TECHNIQUES; CRYSTALLOGRAPHY, X-RAY; DOGS; ENZYME INHIBITORS; HUMANS; LACTAMS; LEUKOCYTE ELASTASE; MALE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRROLES; PYRROLIDINES; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONAMIDES; SWINE;

EID: 0037194629     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm020881f     Document Type: Article

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