- A triazene-based new photolabile linker in solid phase chemistry
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An extension of the T2 linker methodology by showing its applicability as a photocleavable linker is reported. Photocleavage was carried out with 355nm UV laser irradiation (3ω Nd-YAG) in methanol/diethyl ether and is suitable for protected amino acid derivatives, as well as simple small organic molecules including resin-bound biotin. The linker is stable under a wide range of conditions with the exception of strongly acidic media.
- Enders, Dieter,Rijksen, Christiaan,Bremus-K?bberling, Elke,Gillner, Arnold,K?bberling, Johannes
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- Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors
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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.
- Sutton, James C.,Bolton, Scott A.,Hartl, Karen S.,Huang, Ming-Hsing,Jacobs, Glenn,Meng, Wei,Ogletree, Martin L.,Pi, Zulan,Schumacher, William A.,Seiler, Steven M.,Slusarchyk, William A.,Treuner, Uwe,Zahler, Robert,Zhao, Guohua,Bisacchi, Gregory S.
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p. 3229 - 3233
(2007/10/03)
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- Optically active 1,4-dihydropyridine compounds as bradykinin antagonists
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This invention provides a compound of the formula (I): and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo; R1 and R2 are independently C1-4 alkyl; R3 is substituted or unsubstituted, phenyl or naphthyl; Y is heterocyclic group sele
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