Ontology highlight
ABSTRACT:
SUBMITTER: Decker M
PROVIDER: S-EPMC2814335 | biostudies-literature | 2010 Jan
REPOSITORIES: biostudies-literature
Decker Michael M Si Yu-Gui YG Knapp Brian I BI Bidlack Jean M JM Neumeyer John L JL
Journal of medicinal chemistry 20100101 1
The phenolic group of the potent mu and kappa opioid morphinan agonist/antagonists cyclorphan and butorphan was replaced by phenylamino and benzylamino groups including compounds with para-substituents in the benzene ring. These compounds are highly potent mu and kappa ligands, e.g., p-methoxyphenylaminocyclorphan showing a K(i) of 0.026 nM at the mu receptor and a K(i) of 0.03 nM at the kappa receptor. Phenyl carbamates and phenylureas were synthesized and investigated. Selective o-formylation ...[more]