| Title : Benzylidene ketal derivatives as M2 muscarinic receptor antagonists - Boyle_2000_Bioorg.Med.Chem.Lett_10_2727 |
| Author(s) : Boyle CD , Chackalamannil S , Chen LY , Dugar S , Pushpavanam P , Billard W , Binch H, 3rd , Crosby G , Cohen-Williams M , Coffin VL , Duffy RA , Ruperto V , Lachowicz JE |
| Ref : Bioorganic & Medicinal Chemistry Lett , 10 :2727 , 2000 |
|
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. |
| PubMedSearch : Boyle_2000_Bioorg.Med.Chem.Lett_10_2727 |
| PubMedID: 11133078 |
Boyle CD, Chackalamannil S, Chen LY, Dugar S, Pushpavanam P, Billard W, Binch H, 3rd, Crosby G, Cohen-Williams M, Coffin VL, Duffy RA, Ruperto V, Lachowicz JE (2000)
Benzylidene ketal derivatives as M2 muscarinic receptor antagonists
Bioorganic & Medicinal Chemistry Lett
10 :2727
Boyle CD, Chackalamannil S, Chen LY, Dugar S, Pushpavanam P, Billard W, Binch H, 3rd, Crosby G, Cohen-Williams M, Coffin VL, Duffy RA, Ruperto V, Lachowicz JE (2000)
Bioorganic & Medicinal Chemistry Lett
10 :2727