Ontology highlight
ABSTRACT:
SUBMITTER: Moynihan HA
PROVIDER: S-EPMC3506128 | biostudies-literature | 2012 Nov
REPOSITORIES: biostudies-literature
Moynihan Humphrey A HA Derrick Ian I Broadbear Jillian H JH Greedy Benjamin M BM Aceto Mario D MD Harris Louis S LS Purington Lauren C S LC Thomas Mark P MP Woods James H JH Traynor John R JR Husbands Stephen M SM Lewis John W JW
Journal of medicinal chemistry 20121031 22
We have previously shown that cinnamoyl derivatives of 14β-amino-17-cyclopropylmethyl-7,8-dihydronormorphinone and 7α-aminomethyl-6,14-endoethanonororipavine have pronounced pseudoirreversible μ opioid receptor (MOR) antagonism. The present communication describes the synthesis and evaluation of fumaroylamino analogues of these cinnamoylamino derivatives together with some related fumaroyl derivatives. The predominant activity of the new ligands was MOR antagonism. The fumaroylamino analogues (2 ...[more]