1. Synthesis and Structure—Activity Relationships of 8-Azabicyclo[3.2.1]octane Benzylamine NK1 Antagonists
- Author
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Gary G. Chicchi, Marc M. Kurtz, Emma J. Carlson, Alan Wheeldon, Kwei-Lan C. Tsao, Christopher Thomson, Janusz Jozef Kulagowski, and Christopher John Swain
- Subjects
Stereochemistry ,Clinical Biochemistry ,hERG ,Molecular Conformation ,Pharmaceutical Science ,Biochemistry ,Chemical synthesis ,Medicinal chemistry ,Structure-Activity Relationship ,chemistry.chemical_compound ,Benzylamine ,Neurokinin-1 Receptor Antagonists ,Drug Discovery ,Humans ,Structure–activity relationship ,Molecular Biology ,8-azabicyclo(3.2.1)octane benzylamine ,Octane ,Aza Compounds ,Bicyclic molecule ,biology ,Chemistry ,Organic Chemistry ,Stereoisomerism ,General Medicine ,Bridged Bicyclo Compounds, Heterocyclic ,biology.protein ,Molecular Medicine ,NK1 receptor antagonist ,Amine gas treating ,Selectivity - 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.
- Published
- 2006
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