168913-90-4Relevant 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.
New Orally Active Serine Protease Inhibitors: Structural Requirements for Their Good Oral Activity
Senokuchi, Kazuhiko,Nakai, Hisao,Nakayama, Yoshisuke,Odagaki, Yoshihiko,Sakaki, Katsuhito,et al.
, p. 4508 - 4517 (2007/10/03)
Synthesis and structural requirements for good oral activity of a series of para-substituted benzoyl esters of 4-hydroxybenzamidine serine protease inhibitors are described.The structure required for good oral activity was found to be general formula II w
