title: Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.
abstract: A series of tetrahydroquinoline derivatives were synthesized and profiled for their ability to act as glucocorticoid receptor selective modulators. Structure-activity relationships of the tetrahydroquinoline B-ring lead to the discovery of orally available GR-selective agonists with high in vivo activity.
authors.affiliation: Discovery Research, Ligand Pharmaceuticals, La Jolla, CA 92037, USA. andyrhudson@gmail.com
authors.forename: Andrew R
authors.initials: AR
authors.lastname: Hudson
authors.forename: Robert I
authors.initials: RI
authors.lastname: Higuchi
authors.forename: Steven L
authors.initials: SL
authors.lastname: Roach
authors.forename: Mark E
authors.initials: ME
authors.lastname: Adams
authors.forename: Angela
authors.initials: A
authors.lastname: Vassar
authors.forename: Peter M
authors.initials: PM
authors.lastname: Syka
authors.forename: Dale E
authors.initials: DE
authors.lastname: Mais
authors.forename: Jeffrey N
authors.initials: JN
authors.lastname: Miner
authors.forename: Keith B
authors.initials: KB
authors.lastname: Marschke
authors.forename: Lin
authors.initials: L
authors.lastname: Zhi
mesh_terms: D000284:Administration, Oral; D000818:Animals; D055808:Drug Discovery; D004797:Enzyme-Linked Immunosorbent Assay; D006801:Humans; D011804:Quinolines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011965:Receptors, Glucocorticoid / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D011804:Quinolines; D011965:Receptors, Glucocorticoid; C542964:1,2,3,4-tetrahydroquinoline