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  • Title: Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
    Author: 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.
    Journal: J Med Chem; 2002 Dec 05; 45(25):5415-8. PubMed ID: 12459007.
    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.
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