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  • Title: New serine protease inhibitors with leukotriene B4 (LTB4) receptor binding affinity.
    Author: Nakayama Y, Senokuchi K, Sakaki K, Kato M, Maruyama T, Miyazaki T, Ito H, Nakai H, Kawamura M.
    Journal: Bioorg Med Chem; 1997 May; 5(5):971-85. PubMed ID: 9208106.
    Abstract:
    A series of new trypsin-like serine protease inhibitors, 1, 2 and 7-23, containing amidinobenzene moiety was found to show potent LTB4-receptor affinity. Among them, compounds 1 and 2 were found to be LTB4 receptor antagonists based on an inhibition assay of human polymorphonuclear neutrophil (PMN) intracellular calcium mobilization induced by LTB4. Compounds 1 and 2, which satisfy the reported structural requirements for good oral activity, are expected to show a balanced dual mode of action, i.e., protease inhibitory activity and LTB4 receptor antagonist activity, in vivo.
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