2-Aryl Indole NK 1 receptor antagonists: optimisation of indole substitution

…, K Dinnell, JM Elliott, GJ Hollingworth, MM Kurtz…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 9 p. 1233 - 1236

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被引用次数: 59

摘要

The mammalian tachykinin substance P (SP) has been implicated in numerous conditions 1, 2 and 3 including migraine, cystitis, asthma, depression and cytotoxin-induced emesis. This wide range of therapeutic indications has led to the development of various potent antagonists 3 of the receptor to which SP preferentially binds, neurokinin-1 (NK 1 ). Here we report the synthesis and biological activity of a new series of such compounds, concentrating on optimisation ...