C-3 Amido-indole cannabinoid receptor modulators.
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.
Hynes
John
J
Discovery Chemistry, Bristol-Myers Squibb, Princeton, NJ 08543-4000, USA. john.hynes@bms.com
Leftheris
Katerina
K
Wu
Hong
H
Pandit
Chennagiri
C
Chen
Ping
P
Norris
Derek J
DJ
Chen
Bang-Chi
BC
Zhao
Rulin
R
Kiener
Peter A
PA
Chen
Xiaorong
X
Turk
Lori A
LA
Patil-Koota
Vina
V
Gillooly
Kathleen M
KM
Shuster
David J
DJ
McIntyre
Kim W
KW
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
D000577:Amides; D000893:Anti-Inflammatory Agents; D007211:Indoles; D008070:Lipopolysaccharides; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug; D014409:Tumor Necrosis Factor-alpha