title: Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists.
abstract: The design and synthesis of a novel series of Rev-erbα agonists is described. The development and optimization of the tetrahydroisoquinoline series was carried out from an earlier acyclic series of Rev-erbα agonists. Through the optimization of the scaffold 1, several potent compounds with good in vivo profiles were discovered.
authors.affiliation: Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, Jupiter, FL 33458, USA.
authors.forename: Romain
authors.initials: R
authors.lastname: Noel
authors.forename: Xinyi
authors.initials: X
authors.lastname: Song
authors.forename: Youseung
authors.initials: Y
authors.lastname: Shin
authors.forename: Subhashis
authors.initials: S
authors.lastname: Banerjee
authors.forename: Douglas
authors.initials: D
authors.lastname: Kojetin
authors.forename: Li
authors.initials: L
authors.lastname: Lin
authors.forename: Claudia H
authors.initials: CH
authors.lastname: Ruiz
authors.forename: Michael D
authors.initials: MD
authors.lastname: Cameron
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Burris
authors.forename: Theodore M
authors.initials: TM
authors.lastname: Kamenecka
mesh_terms: D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D007274:Injections, Intraperitoneal; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D056953:Nuclear Receptor Subfamily 1, Group D, Member 1 / Q000819:agonists* / Q000378:metabolism; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D007546:Isoquinolines; D009281:Naphthalenes; D056953:Nuclear Receptor Subfamily 1, Group D, Member 1