Author/Authors :
Jason Witherington، نويسنده , , Vincent Bordas، نويسنده , , Dave G. Cooper، نويسنده , , Ian T. Forbes، نويسنده , , Andrew D. Gribble، نويسنده , , Robert J. Ife، نويسنده , , Theo Berkhout، نويسنده , , Jayneeta Gohil، نويسنده , , Pieter H. E. Groot، نويسنده ,
Abstract :
The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. Compared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors.