Publications by authors named "Andy Stocker"
A series of carboxylic acid glycogen phosphorylase inhibitors, which have potential as oral antidiabetic agents, is described. Defining and applying simple physicochemical design criteria was used to assess the opportunity and to focus synthetic efforts on compounds with the greatest probability of success. The study led to compound 17, which exhibits a good balance of properties including potent inhibition of recombinant human liver glycogen phosphorylase in vitro, a good DMPK profile including excellent bioavailability and low clearance and good in vivo activity in a glucagon challenge model of diabetes in Zucker rats.
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- - Two new series of thienopyrrole inhibitors have been developed to target human liver glycogen phosphorylase a (GPa) to help lower glucose production from rat liver cells.
- - These inhibitors work by interacting with a specific site (the dimer interface) in the enzyme's structure, as revealed by X-ray crystallography studies.
- - The research highlights the potential of these compounds in managing glucose levels in the body, which could have implications for diabetes treatment.