177169-07-2Relevant academic research and scientific papers
New serine protease inhibitors with leukotriene B4 (LTB4) receptor binding affinity
Nakayama, Yoshisuke,Senokuchi, Kazuhiko,Sakaki, Katsuhito,Kato, Masashi,Maruyama, Toru,Miyazaki, Toru,Ito, Hidenori,Nakai, Hisao,Kawamura, Masanori
, p. 971 - 985 (2007/10/03)
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.
