Author/Authors :
Joseph Pontillo، نويسنده , , Dongpei Wu، نويسنده , , Brett Ching، نويسنده , , Sarah Hudson، نويسنده , , Marc J. Genicot، نويسنده , , Yinghong Gao، نويسنده , , Todd Ewing، نويسنده , , Beth A. Fleck، نويسنده , , Kathleen Gogas، نويسنده , , Anna Aparicio، نويسنده , , Hua Wang، نويسنده , , Jenny Wen، نويسنده , , Warren S. Wade، نويسنده ,
Abstract :
The design synthesis and SAR of a series of chiral ring-constrained norepinephrine reuptake inhibitors with improved physicochemical properties is described. Typical compounds are potent (IC50s <10 nM), selective against the other monoamine transporters, weak CYP2D6 inhibitors (IC50s > 1 μM) and stable to oxidation by human liver microsomes. In addition, the compounds exhibit a favorable polarity profile.
