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Benzylidene ketal derivatives as M2 muscarinic receptor antagonists
C D Boyle1, S Chackalamannil, L Y Chen
1Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. craig.boyle@spcorp.com
Bioorganic & Medicinal Chemistry Letters
|January 2, 2001
Abstract:
Benzylidene ketal derivatives were investigated as selective M2 receptor antagonists for the treatment of Alzheimer's disease. Compound 10 was discovered to have subnanomolar M2 receptor affinity and 100-fold selectivity against other muscarinic receptors. Also, 10 demonstrated in vivo efficacy in rodent models of muscarinic activity and cognition.