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  • Title: Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.
    Author: Bisacchi GS, Slusarchyk WA, Bolton SA, Hartl KS, Jacobs G, Mathur A, Meng W, Ogletree ML, Pi Z, Sutton JC, Treuner U, Zahler R, Zhao G, Seiler SM.
    Journal: Bioorg Med Chem Lett; 2004 May 03; 14(9):2227-31. PubMed ID: 15081014.
    Abstract:
    Azetidinones such as BMS-363131 (2) and BMS-363130 (3), which contain a guanidine group in the C-3 side chain were previously shown to be very potent inhibitors of human tryptase with high selectivity versus other serine proteases, including trypsin. In this letter, we describe the discovery of a number of potent azetidinone tryptase inhibitors in which the guanidine moiety at the ring C-3 position is replaced with primary or secondary amine or aminopyridine functionality. In particular, BMS-354326 (4) is a highly potent tryptase inhibitor (IC(50)=1.8 nM), which has excellent selectivity against trypsin and most other related serine proteases.
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