Document Report Card

ID: ALA1135669

Journal: J Med Chem

Title: Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.

Authors: Wang Y, Chackalamannil S, Hu Z, Greenlee WJ, Clader J, Boyle CD, Kaminski JJ, Billard W, Binch H, Crosby G, Ruperto V, Duffy RA, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Lachowicz JE.

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.

CiteXplore: 12459007

DOI: 10.1021/jm0255163