Author/Authors :
Richard L. Elliott، نويسنده , , Hana Kopecka، نويسنده , , David E. Gunn، نويسنده , , Nan-Horng Lin، نويسنده , , David S. Garvey، نويسنده , , Keith B. Ryther، نويسنده , , Mark W. Holladay، نويسنده , , David J. Anderson، نويسنده , , Jeffrey E. Campbell، نويسنده , , James P. Sullivan، نويسنده , , Michael J. Buckley، نويسنده , , Karen L. Gunther، نويسنده , , Alyssa B. OʹNeill، نويسنده , , Michael W. Decker، نويسنده , , Stephen P. Arneri ، نويسنده ,
Abstract :
A series of 2-(aryloxymethyl) azetidine and pyrrolidine nAChR ligands in which the 3-pyridyl moiety of a previously described series1 was replaced by a substituted phenyl group was explored. Aromatic substitution afforded analogues with Ki values ranging from 3 to>10,000 nM. Generally, substitution at the ortho- and para-position was unfavorable, whereas electron-withdrawing groups at the meta-position improved the Ki values.