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.
|Number of pages||4|
|Journal||Bioorganic and Medicinal Chemistry Letters|
|Publication status||Published - 20 Aug 2001|