Ontology highlight
ABSTRACT:
SUBMITTER: Amato G
PROVIDER: S-EPMC7656562 | biostudies-literature | 2019 Jul
REPOSITORIES: biostudies-literature
Amato George G Manke Amruta A Wiethe Robert R Vasukuttan Vineetha V Snyder Rodney R Yueh Yun Lan YL Decker Ann A Runyon Scott S Maitra Rangan R
Journal of medicinal chemistry 20190622 13
Peripherally restricted CB1 receptor antagonists may be useful in treating metabolic syndrome, diabetes, liver diseases, and gastrointestinal disorders. Clinical development of the centrally acting CB1 inverse agonist otenabant (<b>1</b>) was halted due to its potential of producing adverse effects. SAR studies of <b>1</b> are reported herein with the objective of producing peripherally restricted analogues. Crystal structures of hCB1 and docking studies with <b>1</b> indicate that the piperidin ...[more]