title: Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.
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.
authors.affiliation: Neuroscience Research, GPRD, Abbott, Abbott Park, IL 60064-6117, USA. Tao.Li@abbott.com
authors.forename: Tao
authors.initials: T
authors.lastname: Li
authors.forename: William H
authors.initials: WH
authors.lastname: Bunnelle
authors.forename: Keith B
authors.initials: KB
authors.lastname: Ryther
authors.forename: David J
authors.initials: DJ
authors.lastname: Anderson
authors.forename: John
authors.initials: J
authors.lastname: Malysz
authors.forename: Rosalind
authors.initials: R
authors.lastname: Helfrich
authors.forename: Jens H
authors.initials: JH
authors.lastname: Grønlien
authors.forename: Monika
authors.initials: M
authors.lastname: Håkerud
authors.forename: Dan
authors.initials: D
authors.lastname: Peters
authors.forename: Michael R
authors.initials: MR
authors.lastname: Schrimpf
authors.forename: Murali
authors.initials: M
authors.lastname: Gopalakrishnan
authors.forename: Jianguo
authors.initials: J
authors.lastname: Ji
mesh_terms: D000818:Animals; D006536:Heptanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D009474:Neurons / Q000378:metabolism; D018722:Nicotinic Agonists / Q000138:chemical synthesis / Q000737:chemistry*; D011485:Protein Binding; D011869:Radioligand Assay; D051381:Rats; D011978:Receptors, Nicotinic / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D006536:Heptanes; D008024:Ligands; D018722:Nicotinic Agonists; D011978:Receptors, Nicotinic