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1: Bioorg Med Chem Lett. 2006 Feb 15;16(4):811-4. Epub 2005 Nov 22.Click here to read Links

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

Thomson CG, Carlson E, Chicchi GG, Kulagowski JJ, Kurtz MM, Swain CJ, Tsao KL, Wheeldon 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.

PMID: 16307878 [PubMed - indexed for MEDLINE]

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