Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
作者信息
Wang Yuguang, Chackalamannil Samuel, Hu Zhiyong, Greenlee William J, Clader John, Boyle Craig D, Kaminski James J, Billard William, Binch Herbert, Crosby Gordon, Ruperto Vilma, Duffy Ruth A, Cohen-Williams Mary, Coffin Vicki L, Cox Kathleen A, Grotz Diane E, Lachowicz Jean E
机构信息
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA.
出版信息
J Med Chem. 2002 Dec 5;45(25):5415-8. doi: 10.1021/jm0255163.
PMID: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.
摘要
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