Literature DB >> 20472430

Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.

Tao Li1, William H Bunnelle, Keith B Ryther, David J Anderson, John Malysz, Rosalind Helfrich, Jens H Grønlien, Monika Håkerud, Dan Peters, Michael R Schrimpf, Murali Gopalakrishnan, Jianguo Ji.   

Abstract

Biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes have been synthesized and tested for their affinity toward alpha7 neuronal nicotinic receptors (NNRs). SAR studies established that 5-N-methyl substituent, heteroaryl linker and the nature of terminal aryl group are critical for the ligand to achieve potent alpha7 NNR agonist activity. Copyright 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2010        PMID: 20472430     DOI: 10.1016/j.bmcl.2010.04.105

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


  3 in total

1.  5-(5-(6-[(11)C]methyl-3,6-diazabicyclo[3.2.0]heptan-3-yl)pyridin-2-yl)-1H-indole as a potential PET radioligand for imaging cerebral α7-nAChR in mice.

Authors:  Yongjun Gao; Hayden T Ravert; Heather Valentine; Ursula Scheffel; Paige Finley; Dean F Wong; Robert F Dannals; Andrew G Horti
Journal:  Bioorg Med Chem       Date:  2012-05-04       Impact factor: 3.641

2.  (1S,4S)-2-(2,4-Difluoro-phen-yl)-5-[(4-methyl-phen-yl)sulfon-yl]-2,5-diaza-bicyclo-[2.2.1]hepta-ne.

Authors:  Chunli Wu; Jingyu Zhang; Pan Li; Junxia Zhang; Jizhou Wu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-01-08

3.  Crystal structure of (1S,4S)-2,5-diazo-niabi-cyclo[2.2.1]heptane dibromide.

Authors:  Sergey N Britvin; Andrey M Rumyantsev
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2017-11-17
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.