Details

Autor(en) / Beteiligte

• 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

Titel

2-Aryl indole NK 1 receptor antagonists: optimisation of the 2-Aryl ring and the indole nitrogen substituent

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2001, Vol.11 (9), p.1237-1240

Ort / Verlag

Elsevier Ltd

Erscheinungsjahr

2001

Link zum Volltext

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• Novel 2-aryl indole hNK 1 receptor ligands were prepared utilising palladium cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK 1 receptor binding affinity and good brain penetration (e.g., 9d) were synthesised. Graphic