Bioorganic and Medicinal Chemistry Letters p. 2727 - 2730 (2000)
Update date:2022-09-26
Topics: Derivatives binding affinity Antagonists Chemical Synthesis High-Throughput Screening M2 muscarinic receptor
Boyle, Craig D
Chackalamannil, Samuel
Chen, Lian-Yong
Dugar, Sundeep
Pushpavanam, Pradeep
Billard, William
Binch III, Herbert
Crosby, Gordon
Cohen-Williams, Mary
Coffin, Vicki L
Duffy, Ruth A
Ruperto, Vilma
Lachowicz, Jean E
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. (C) 2000 Elsevier Science Ltd.
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