Author/Authors :
Yoshisuke Nakayama، نويسنده , , Kazuhiko Senokuchi، نويسنده , , Katsuhito Sakaki، نويسنده , , Masashi Kato، نويسنده , , Toru Maruyama، نويسنده , , Toru Miyazaki، نويسنده , , Hidenori Ito، نويسنده , , Hisao Nakai، نويسنده , , Masanori Kawamura، نويسنده ,
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.
