Bioorganic & Medicinal Chemistry Letters 2001-08-20

Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.

J Witherington, V Bordas, D G Cooper, I T Forbes, A D Gribble, R J Ife, T Berkhout, J Gohil, P H Groot

Index: Bioorg. Med. Chem. Lett. 11(16) , 2177-80, (2001)

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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.