Ontology highlight
ABSTRACT:
SUBMITTER: Henry S
PROVIDER: S-EPMC7047604 | biostudies-literature | 2020 Feb
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20200210 4
We previously reported a novel SAR campaign that converted a metabolically unstable series of μ-opioid receptor (MOR) agonist/δ-opioid receptor (DOR) antagonist bicyclic core peptidomimetics with promising analgesic activity and reduced abuse liabilities into a more stable series of benzylic core analogues. Herein, we expanded the SAR of that campaign and determined that the incorporation of amines into the benzylic pendant produces enhanced MOR-efficacy in this series, whereas the reincorporati ...[more]