Tetrahydroquinoline derivatives as CRTH2 antagonists
A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 an
Liu, Jiwen,Wang, Yingcai,Sun, Ying,Marshall, Derek,Miao, Shichang,Tonn, George,Anders, Penny,Tocker, Joel,Tang, H. Lucy,Medina, Julio
scheme or table
p. 6840 - 6844
(2010/05/19)
Synthesis and SAR of cis-1-Benzoyl-1,2,3,4-tetrahydroquinoline ligands for control of gene expression in ecdysone responsive systems
A library of 35 cis-1-benzoyl-2-methyl-4-(phenylamino)-1,2,3,4-tetrahydroquinolines was prepared. The compounds bore various substitutuents on the benzoyl ring, at the 4-position of the phenylamino ring and at the 6-position of the tetrahydroquinoline rin
Smith, Howard C.,Cavanaugh, Caitlin K.,Friz, Jennifer L.,Thompson, Christine S.,Saggers, Jessica A.,Michelotti, Enrique L.,Garcia, Javier,Tice, Colin M.