Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

Jason Witherington, Vincent Bordas, Dave G. Cooper, Ian T. Forbes, Andrew D. Gribble, Robert J. Ife, Theo Berkhout, Jayneeta Gohil, Pieter H. E. Groot

Research output: Contribution to journalArticlepeer-review

46 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)2177-2180
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number16
Publication statusPublished - 20 Aug 2001


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