bms-262084 and Asthma
bms-262084 has been researched along with Asthma* in 2 studies
Other Studies
2 other study(ies) available for bms-262084 and Asthma
| Article | Year |
|---|---|
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
A series of N1-activated C4-carboxy azetidinones was prepared and tested as inhibitors of human tryptase. The key stereochemical and functional features required for potency, serine protease specificity and aqueous stability were determined. From these studies compound 2, BMS-262084, was identified as a potent and selective tryptase inhibitor which, when dosed intratracheally in ovalbumin-sensitized guinea pigs, reduced allergen-induced bronchoconstriction and inflammatory cell infiltration into the lung. Topics: Animals; Anti-Asthmatic Agents; Asthma; Azetidines; Bronchoconstriction; Crystallography, X-Ray; Extracellular Space; Guinea Pigs; Half-Life; Humans; Inflammation; Lung; Molecular Conformation; Ovalbumin; Piperazines; Serine Endopeptidases; Serine Proteinase Inhibitors; Structure-Activity Relationship; Tryptases | 2002 |
Synthesis of potent and highly selective inhibitors of human tryptase.
The serine protease tryptase has been implicated in allergic and inflammatory diseases and associated with asthma. The synthesis and SAR of a series of N1-activated-4-carboxy azetidinones are described, resulting in identification of BMS-363131 (2) as a potent inhibitor of human tryptase (IC(50)<1.7 nM) with high selectivity (>3000-fold) for tryptase versus related serine proteases including trypsin. Topics: Animals; Anti-Asthmatic Agents; Asthma; Azetidines; Aziridines; Drug Stability; Guinea Pigs; Humans; Ovalbumin; Piperazines; Serine Endopeptidases; Serine Proteinase Inhibitors; Stereoisomerism; Structure-Activity Relationship; Tryptases | 2002 |