Author/Authors :
Gilles C. Bignan، نويسنده , , Kathleen Battista، نويسنده , , Peter J. Connolly، نويسنده , , Michael J. Orsini، نويسنده , , Jingchun Liu، نويسنده , , Steven A. Middleton، نويسنده , , Allen B. Reitz، نويسنده ,
Abstract :
A novel series of indolin-2-ones having a spirocyclic piperidine ring at the 3-position was synthesized and found to bind with high affinity to the ORL-1 receptor. Structure–activity relationships at the piperidine nitrogen were investigated. Substitution on the phenyl ring and nitrogen atom of the indolin-2-one core generated several selective high-affinity ligands that were antagonists of the ORL-1 receptor.