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.
Department of Chemistry, University of Leicester, Leicester LE1 7RH, United Kingdom. anup.patel@pera.com
Anup B
AB
Patel
John R
JR
Malpass
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