New serine protease inhibitors with leukotriene B 4 (LTB 4) receptor binding affinity

Y Nakayama, K Senokuchi, K Sakaki, M Kato…

Index: Nakayama, Yoshisuke; Senokuchi, Kazuhiko; Sakaki, Katsuhito; Kato, Masashi; Maruyama, Toru; Miyazaki, Toru; Ito, Hidenori; Nakai, Hisao; Kawamura, Masanori Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 5 p. 971 - 985

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Citation Number: 9

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 ...