B. Le Bourdonnec, S. Belanger, J. Cassel
Dec 15, 2003
Citations
2
Influential Citations
18
Citations
Journal
Bioorganic & medicinal chemistry letters
Abstract
trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines constitute a novel class of micro opioid receptor antagonists. The CONH(2) group was found to be an effective isostere of the phenolic OH moiety. Structure-activity relationships at the piperidine nitrogen position led to the identification of several ligands displaying high affinity toward the cloned human micro opioid receptors, good selectivity micro/delta, micro/kappa, and potent in vitro antagonist activity.