title: C-3 Amido-indole cannabinoid receptor modulators.
abstract: C-3 Amido-indoles were found to selectively bind to the CB2 receptor. SAR studies led to optimized compounds with excellent in vivo potency against LPS induced TNF-alpha release in murine models of cytokine production.
authors.affiliation: Discovery Chemistry, Bristol-Myers Squibb, Princeton, NJ 08543-4000, USA. john.hynes@bms.com
authors.forename: John
authors.initials: J
authors.lastname: Hynes
authors.forename: Katerina
authors.initials: K
authors.lastname: Leftheris
authors.forename: Hong
authors.initials: H
authors.lastname: Wu
authors.forename: Chennagiri
authors.initials: C
authors.lastname: Pandit
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Derek J
authors.initials: DJ
authors.lastname: Norris
authors.forename: Bang-Chi
authors.initials: BC
authors.lastname: Chen
authors.forename: Rulin
authors.initials: R
authors.lastname: Zhao
authors.forename: Peter A
authors.initials: PA
authors.lastname: Kiener
authors.forename: Xiaorong
authors.initials: X
authors.lastname: Chen
authors.forename: Lori A
authors.initials: LA
authors.lastname: Turk
authors.forename: Vina
authors.initials: V
authors.lastname: Patil-Koota
authors.forename: Kathleen M
authors.initials: KM
authors.lastname: Gillooly
authors.forename: David J
authors.initials: DJ
authors.lastname: Shuster
authors.forename: Kim W
authors.initials: KW
authors.lastname: McIntyre
mesh_terms: D000577:Amides; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D007111:Immunity, Cellular / Q000187:drug effects; D007211:Indoles; D020128:Inhibitory Concentration 50; D007963:Leukocytes, Mononuclear / Q000187:drug effects / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology; D051379:Mice; D011485:Protein Binding; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000819:agonists*; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000378:metabolism
chemical_list: D000577:Amides; D000893:Anti-Inflammatory Agents; D007211:Indoles; D008070:Lipopolysaccharides; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; D014409:Tumor Necrosis Factor-alpha