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Abstract
Novelty: A series of azabicyclo oximes are claimed. These compounds are stated to be selective MI muscarinic agonists and their use for alleviating pain and treatment of the symptoms of cognitive decline is also claimed.
Biology: Binding data are given using the method of Watson et al. (J. Pharmacol. Exp. Ther (1986) 237:411) for RQNB binding and the method of Vickroy et a f . (J . Pharrnacof. Exp. Ther: (1984) 229:747) for RCMD binding. A range of IC50 values are given (0.15-218 nM for RCMD and 44-17658nM for RQND binding) showing MI selectivity.
Chemistry: The oximes are prepared using standard chemistry starting from the 1-azabicyclo[2.2.11 hept-3-one and a hydroxylamine. Over fifty compounds are claimed including Z-(+)- 1 -azabicyclo[2.2.1] heptan-3-one,O-(Z-3-methyl-5-phenyl-2-penten-4-ynyl)oxime oxalate.