New serine protease inhibitors with leukotriene B4 (LTB4) receptor binding affinity

Article abstract of DOI:10.1016/S0968-0896(97)00036-9

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.