Literature DB >> 12459007

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

Yuguang Wang1, Samuel Chackalamannil, Zhiyong Hu, William J Greenlee, John Clader, Craig D Boyle, James J Kaminski, William Billard, Herbert Binch, Gordon Crosby, Vilma Ruperto, Ruth A Duffy, Mary Cohen-Williams, Vicki L Coffin, Kathleen A Cox, Diane E Grotz, Jean E Lachowicz.   

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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Year:  2002        PMID： 12459007     DOI： 10.1021/jm0255163

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  2 in total

1.  In vivo brain microdialysis: advances in neuropsychopharmacology and drug discovery.

Authors:  Altaf S Darvesh; Richard T Carroll; Werner J Geldenhuys; Gary A Gudelsky; Jochen Klein; Charles K Meshul; Cornelis J Van der Schyf
Journal:  Expert Opin Drug Discov       Date:  2011-02       Impact factor: 6.098

2.  Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.

Authors:  Guangrong Zheng; Andrew M Smith; Xiaoqin Huang; Karunai L Subramanian; Kiran B Siripurapu; Agripina Deaciuc; Chang-Guo Zhan; Linda P Dwoskin
Journal:  J Med Chem       Date:  2013-02-18       Impact factor: 7.446
  2 in total

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