Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors
A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and physical-chemical properties. Several highly potent compounds such as 8ji, 8jl, and 8jm were identified with single nanomolar activities. The most potent compound 8jm showed an IC50 of 3 nM, lower microsome clearance and no CYP inhibition. The profile of 8jm appeared to be superior to BMS433771, and supported further optimization.
Feng, Song,Hong, Di,Wang, Baoxia,Zheng, Xiufang,Miao, Kun,Wang, Lisha,Yun, Hongying,Gao, Lu,Zhao, Shuhai,Shen, Hong C.
The present invention provides a compound of a formula (I), wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE4 mediated disease state.
-
Page/Page column 149
(2008/12/07)
CHEMICAL COMPOUNDS 635 : PYRIDOPYRIMIDINEDIONES AS PDE4 INHIBITORS
The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE 4 mediated disease state.
-
Page/Page column 38
(2008/12/07)
More Articles about upstream products of 1038827-63-2