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ID: ALA1134265
Journal: Bioorg Med Chem Lett
Title: 2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.
Authors: Dinnell K, Chicchi GG, Dhar MJ, Elliott JM, Hollingworth GJ, Kurtz MM, Ridgill MP, Rycroft W, Tsao KL, Williams AR, Swain CJ.
Abstract: 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.
CiteXplore: 11354385