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

Bioorganic & medicinal chemistry letters 2006 Feb 15; 16(4):811-4

Link to PubMed abstract

Thomson C CG, Carlson E E, Chicchi G GG, Kulagowski J JJ, Kurtz M MM, Swain C CJ, Tsao K KL, Wheeldon A A

Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK. christopher_thomson@merck.com

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.