2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution

L C Cooper; G G Chicchi; K Dinnell; J M Elliott; G J Hollingworth; M M Kurtz; K L Locker; D Morrison; D E Shaw; K L Tsao; A P Watt; A R Williams; C J Swain

doi:10.1016/s0960-894x(01)00182-2

2-Aryl indole NK1 receptor antagonists: optimisation of indole substitution

Bioorg Med Chem Lett. 2001 May 7;11(9):1233-6. doi: 10.1016/s0960-894x(01)00182-2.

Authors

L C Cooper¹, G G Chicchi, K Dinnell, J M Elliott, G J Hollingworth, M M Kurtz, K L Locker, D Morrison, D E Shaw, K L Tsao, A P Watt, A R Williams, C J Swain

Affiliation

¹ Department of Medicinal Chemistry, The Neuroscience Research Centre, Harlow, Essex, UK. laura_cooper@merck.com

PMID: 11354384
DOI: 10.1016/s0960-894x(01)00182-2

Abstract

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.

MeSH terms

Animals
Behavior, Animal
Binding, Competitive / drug effects
Brain Chemistry
CHO Cells
Cricetinae
Gerbillinae
Indicators and Reagents
Indoles / chemical synthesis*
Indoles / pharmacokinetics
Indoles / pharmacology*
Neurokinin-1 Receptor Antagonists*
Rats
Structure-Activity Relationship
Substance P / metabolism

Substances

Indicators and Reagents
Indoles
Neurokinin-1 Receptor Antagonists
Substance P