Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 6, 2008, Pages 2114-2121

  Costanzo, Michael J ^a   Yabut, Stephen C ^a   Zhang, Han Cheng ^a   White, Kimberley B ^a   de Garavilla, Lawrence ^a   Wang, Yuanping ^a   Minor, Lisa K ^a   Tounge, Brett A ^a   Barnakov, Alexander N ^a   Lewandowski, Frank ^a   Milligan, Cynthia ^a   Spurlino, John C ^a   Abraham, William M ^b   Boswell Smith, Victoria ^c   Page, Clive P ^c   Maryanoff, Bruce E ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

^b UNIVERSITY OF MIAMI   (United States)

^c KING'S COLLEGE LONDON   (United Kingdom)

Author keywords

Asthma; Inhibitor; Spiropiperidine; Tryptase

Indexed keywords

AMIDE; JNJ 27390467; MONOMER; PIPERIDINE DERIVATIVE; TETRAMER; TRYPTASE INHIBITOR; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; ASTHMA; CONTROLLED STUDY; CRYSTAL STRUCTURE; DISEASE MODEL; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVE SITE; ENZYME INHIBITION; GUINEA PIG; HYDROPHOBICITY; IC 50; LIVER MICROSOME; NONHUMAN; REACTION ANALYSIS; RESPIRATORY TRACT INFLAMMATION; SHEEP; STRUCTURE ANALYSIS;

ADMINISTRATION, ORAL; ANIMALS; ASTHMA; BIOLOGICAL AVAILABILITY; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CRYSTALLOGRAPHY, X-RAY; CYTOCHROME P-450 ENZYME SYSTEM; DISEASE MODELS, ANIMAL; DOGS; GUINEA PIGS; HUMANS; MICROSOMES, LIVER; MOLECULAR STRUCTURE; RATS; RESPIRATORY HYPERSENSITIVITY; SERINE PROTEINASE INHIBITORS; SHEEP; SPECTROMETRY, MASS, ELECTROSPRAY IONIZATION; SPIRO COMPOUNDS; TRYPSIN; TRYPTASES;

ANIMALIA; CAVIA; OVIS ARIES;

EID: 40749086016     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.01.093     Document Type: Article

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