Bioorganic and Medicinal Chemistry Letters p. 1023 - 1028 (2003)
Update date:2022-08-05
Topics:
Quan, Mimi L.
Ellis, Christopher D.
He, Ming Y.
Liauw, Ann Y.
Lam, Patrick Y. S.
Rossi, Karen A.
Knabb, Robert M.
Luettgen, Joseph M.
Wright, Matthew R.
Wong, Pancras C.
Wexler, Ruth R.
Factor Xa (fXa) is an important serine protease in the blood coagulation cascade. Inhibition of fXa has emerged as an attractive target for potential therapeutic applications in the treatments of both arterial and venous thrombosis. Herein, we describe a series of non-benzamidine isoxazoline derivatives as fXa inhibitors. The chloroaniline group was found to be the most potent benzamidine mimic in this series. Chloroaniline 1 (ST368) has a Ki value of 1.5 nM against fXa and is highly selective for fXa relative to thrombin and trypsin.
View MoreHangzhou Gangjin Chemical Co.,Ltd.
Contact:+86-571-85109780
Address:707 Zhejiang Minhang Bldg., No.290 Zhongshan North Road, Hangzhou 310003, China
Sichuan Highlight Fine Chemicals Co., Ltd.
Contact:+86-28-8525 1605
Address:A5-102 Airport base,388 West Airport Huang He Zhong Lu,2 Section
Shanghai Harvest Chemical Ind. Co., Ltd.
Contact:021-51385350
Address:ROOM 806-807, AI LI CHEN BUILDING, No.333 JINGXIANG ROAD, PUDONG DISTRICT, 201206, SHANGHAI
Dongtai Xinyuan Chemical Co., Ltd.
Contact:+86-21-56733000
Address:404F, 99Nong No.117 Zhongtan Rd. Shanghai
Contact:86-0510-85133006
Address:hubin road NO157
Doi:10.1016/0040-4020(77)80095-1
(1977)Doi:10.1248/cpb.25.1443
(1977)Doi:10.1039/b401792g
(2004)Doi:10.1016/S0008-6215(00)83180-8
(1977)Doi:10.1016/j.tet.2003.11.003
(2004)Doi:10.1021/ja00477a047
(1978)