Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists

  • Bioorg Med Chem Lett. 2006 Feb 15;16(4):811-4. doi: 10.1016/j.bmcl.2005.11.026.
Christopher G Thomson  1 ,  Emma Carlson ,  Gary G Chicchi ,  Janusz J Kulagowski ,  Marc M Kurtz ,  Christopher J Swain ,  Kwei-Lan C Tsao ,  Alan Wheeldon
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK. [email protected]
PMID: 16307878 DOI: 10.1016/j.bmcl.2005.11.026
Abstract

A series of 8-azabicyclo[3.2.1]octane amine hNK1 antagonists has been investigated and structure-activity relationships of the benzylamine and 6-exo substituents described. Acidic substituents at C6 give a series of high affinity compounds for hNK1 with selectivity over the hERG channel.