Benzylidene Ketal Derivatives As M-2 Muscarinic Receptor Antagonists.

Benzylidene ketal derivatives were investigated as selective M-2 receptor antagonists for the treatment of Alzheimer's disease. Compound 10 was discovered to have subnanomolar M-2 receptor affinity and 100-fold selectivity against other muscarinic receptors. Also, 10 demonstrated in vivo efficacy in rodent models of muscarinic activity and cognition. (C) 2000 Elsevier Science Ltd. All rights reserved.