2. Academic Validation
  3. Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists

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

Affiliation

  • 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.

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