| Title : Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists - Wang_2002_J.Med.Chem_45_5415 |
| Author(s) : Wang Y , Chackalamannil S , Hu Z , Greenlee WJ , Clader J , Boyle CD , Kaminski JJ , Billard W , Binch H, 3rd , Crosby G , Ruperto V , Duffy RA , Cohen-Williams M , Coffin VL , Cox KA , Grotz DE , Lachowicz JE |
| Ref : Journal of Medicinal Chemistry , 45 :5415 , 2002 |
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Abstract :
In search of a backup M(2) muscarinic receptor antagonist to the previously reported compound 1, we discovered compound (+)-14, which showed superior oral efficacy in animal models. The improvement of oral efficacy was achieved by modulating both the molecular weight and lipophilicity of the lead compounds. |
| PubMedSearch : Wang_2002_J.Med.Chem_45_5415 |
| PubMedID: 12459007 |
Wang Y, Chackalamannil S, Hu Z, Greenlee WJ, Clader J, Boyle CD, Kaminski JJ, Billard W, Binch H, 3rd, Crosby G, Ruperto V, Duffy RA, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Lachowicz JE (2002)
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists
Journal of Medicinal Chemistry
45 :5415
Wang Y, Chackalamannil S, Hu Z, Greenlee WJ, Clader J, Boyle CD, Kaminski JJ, Billard W, Binch H, 3rd, Crosby G, Ruperto V, Duffy RA, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Lachowicz JE (2002)
Journal of Medicinal Chemistry
45 :5415