290831-92-4Relevant academic research and scientific papers
2-Aryl indole NK1 receptor antagonists: Optimisation of indole substitution
Cooper, Laura C.,Chicchi, Gary G.,Dinnell, Kevin,Elliott, Jason M.,Hollingworth, Gregory J.,Kurtz, Marc M.,Locker, Karen L.,Morrison, Denise,Shaw, Duncan E.,Tsao, Kwei-Lan,Watt, Alan P.,Williams, Angela R.,Swain, Christopher J.
, p. 1233 - 1236 (2007/10/03)
The synthesis and biological evaluation of a series of 2-aryl indoles with high affinity for the human neurokinin-1 (hNK1) receptor are reported, concentrating on optimisation of the indole substitution.
2-Aryl indole NK1 receptor antagonists: Optimisation of the 2-aryl ring and the indole nitrogen substituent
Dinnell, Kevin,Chicchi, Gary G.,Dhar, Madhumeeta J.,Elliott, Jason M.,Hollingworth, Gregory J.,Kurtz, Marc M.,Ridgill, Mark P.,Rycroft, Wayne,Tsao, Kwei-Lan,Williams, Angela R.,Swain, Christopher J.
, p. 1237 - 1240 (2007/10/03)
Novel 2-aryl indole hNK1 receptor ligands were prepared utilising palladium cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK1 receptor binding affinity and good brain penetration (e.g., 9d) were synthesised.
