title: Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists.
abstract: Novel indole-propionic acid derivatives were developed as sphingosine-1-phosphate (S1P) receptor agonists through a systematic SAR study. The optimized and S1P(3) selective S1P(1) agonist 9f induced peripheral blood lymphocyte reduction in vivo and has an excellent efficacy in mouse experimental autoimmune encephalomyelitis (EAE).
authors.affiliation: Research and Development, GlaxoSmithKline Pharmaceuticals, Pudong, Shanghai, China.
authors.forename: Qinghua
authors.initials: Q
authors.lastname: Meng
authors.forename: Baowei
authors.initials: B
authors.lastname: Zhao
authors.forename: Qiongfeng
authors.initials: Q
authors.lastname: Xu
authors.forename: Xuesong
authors.initials: X
authors.lastname: Xu
authors.forename: Guanghui
authors.initials: G
authors.lastname: Deng
authors.forename: Chengyong
authors.initials: C
authors.lastname: Li
authors.forename: Linbo
authors.initials: L
authors.lastname: Luan
authors.forename: Feng
authors.initials: F
authors.lastname: Ren
authors.forename: Hailong
authors.initials: H
authors.lastname: Wang
authors.forename: Heng
authors.initials: H
authors.lastname: Xu
authors.forename: Yan
authors.initials: Y
authors.lastname: Xu
authors.forename: Haibo
authors.initials: H
authors.lastname: Zhang
authors.forename: Jia-Ning
authors.initials: JN
authors.lastname: Xiang
authors.forename: John D
authors.initials: JD
authors.lastname: Elliott
authors.forename: Taylor B
authors.initials: TB
authors.lastname: Guo
authors.forename: Yonggang
authors.initials: Y
authors.lastname: Zhao
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.forename: Hongtao
authors.initials: H
authors.lastname: Lu
authors.forename: Xichen
authors.initials: X
authors.lastname: Lin
mesh_terms: D000818:Animals; D015536:Down-Regulation / Q000187:drug effects; D004681:Encephalomyelitis, Autoimmune, Experimental / Q000628:therapy; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology; D008214:Lymphocytes / Q000166:cytology / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D011422:Propionates / Q000737:chemistry* / Q000494:pharmacology; D049349:Receptors, Lysosphingolipid / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D011422:Propionates; D049349:Receptors, Lysosphingolipid; C029658:propionic acid