Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists
Author
Witherington, Jason
Bordas, Vincent
Cooper, Dave G.
Forbes, Ian T.
Gribble, Andrew D.
Ife, Robert J.
Berkhout, Theo
Gohil, Jayneeta
Groot, Pieter H. E.
Attention
2299/13698
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.