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ID: ALA1132840

Journal: Bioorg Med Chem Lett

Title: Benzylidene ketal derivatives as M2 muscarinic receptor antagonists.

Authors: Boyle CD, Chackalamannil S, Chen LY, Dugar S, Pushpavanam P, Billard W, Binch H, Crosby G, Cohen-Williams M, Coffin VL, Duffy RA, Ruperto V, Lachowicz JE.

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.

CiteXplore: 11133078

DOI: 10.1016/s0960-894x(00)00553-9