Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists
Witherington, Jason, Bordas, Vincent, Cooper, Dave G., Forbes, Ian T., Gribble, Andrew D., Ife, Robert J., Berkhout, Theo, Gohil, Jayneeta and Groot, Pieter H. E.
(2001)
Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.
Bioorganic and Medicinal Chemistry Letters (16).
pp. 2177-2180.
ISSN 0960-894X
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.
| Item Type | Article |
|---|---|
| Subjects |
Biochemistry, Genetics and Molecular Biology(all) > Biochemistry Biochemistry, Genetics and Molecular Biology(all) > Molecular Biology Chemistry(all) > Organic Chemistry Pharmacology, Toxicology and Pharmaceutics(all) > Drug Discovery Pharmacology, Toxicology and Pharmaceutics(all) > Pharmaceutical Science |
| Date Deposited | 29 May 2025 09:06 |
| Last Modified | 29 May 2025 09:06 |