Author/Authors :
David Bolton، نويسنده , , Izzy Boyfield، نويسنده , , Martyn C. Coldwell، نويسنده , , Michael S. Hadley، نويسنده , , Maureen A. M. Healy، نويسنده , , Christopher N. Johnson، نويسنده , , Roger E. Markwell، نويسنده , , David J. Nash، نويسنده , , Graham J. Riley، نويسنده , , Geoffrey Stemp، نويسنده , , Harry J. Wadsworth، نويسنده ,
Abstract :
A series of 2,5-disubstituted-1H-pyrroles (4–18) has been prepared based on replacement of the amide of sultopride 1 by a pyrrole ring. Subsequent modification of the basic side chain gave compounds with high affinity for the dopamine D3 receptor. In addition, 12 and 17 were shown to be D3 antagonists with 30-fold selectivity for the D3 receptor over the D2 receptor.