Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists

J Witherington, V Bordas, DG Cooper, IT Forbes…

文献索引：Witherington, Jason; Bordas, Vincent; Cooper, Dave G.; Forbes, Ian T.; Gribble, Andrew D.; Ife, Robert J.; Berkhout, Theo; Gohil, Jayneeta; Groot, Pieter H.E. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 16 p. 2177 - 2180

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被引用次数: 44

摘要

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.