Potential nicotinic acetylcholine receptor ligands from 2,4-methanoproline derivatives.
Potential nicotinic acetylcholine receptor (nAChR) ligands have been synthesized in which a methylisoxazole substituent is attached to the 1-position ( 26) of the 2-azabicyclo[2.1.1]hexane ring system or separated by "spacer" atoms ( 21 and 23). With ABT-594 as a model, a range of pyridine heterocycles have been attached to the 1-position via a -CH 2O- spacer ( 11, 14, and 6). The biological evaluation of target compounds showed there was no binding affinity at the alpha4beta2 and alpha3beta4 nAChR subtypes.
Patel
Anup B
AB
Department of Chemistry, University of Leicester, Leicester LE1 7RH, United Kingdom. anup.patel@pera.com
Malpass
John R
JR
D002460:Cell Line; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D018722:Nicotinic Agonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011392:Proline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011978:Receptors, Nicotinic / Q000378:metabolism*; D013329:Structure-Activity Relationship
C450189:2,4-methanoproline; D008024:Ligands; D018722:Nicotinic Agonists; D011978:Receptors, Nicotinic; D011392:Proline