Literature DB >> 10843217

Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor.

J Lee1, C B Davis, R A Rivero, A B Reitz, R P Shank.   

Abstract

The preparation of novel pyridyl ethers as ligands for the nicotinic acetylcholine receptor (nAChR) is described. Variations of the ring size of the azacycle and substitution on the pyridine had dramatic effects on receptor binding affinity with IC50s at the alpha4beta2 nAChR ranging from 22 to >10,000 nM. The most potent molecule was (R)-2-chloro-3-(4-cyanophenyl)-5-((3-pyrrolidinyl)oxy)pyridine 27f with an IC50 of 22 nM.

Entities:  

Mesh:

Substances:

Year:  2000        PMID: 10843217     DOI: 10.1016/s0960-894x(00)00168-2

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2(*) and alpha7(*) neuronal nicotinic acetylcholine receptors.

Authors:  Jianhong Chen; Seth Norrholm; Linda P Dwoskin; Peter A Crooks; Donglu Bai
Journal:  Bioorg Med Chem Lett       Date:  2003-01-06       Impact factor: 2.823

  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.