Emma L. Kaplan

TL;DR: Methyl substitution of the piperazine at the 2- and 5-positions markedly increased the potency of the lead compound (>1,000-fold) and oral bioavailability of the compounds in this series is good and is optimal when the 4-position of thepiperazine is substituted with an electron-poor benzoyl moiety.

TL;DR: Small electron-withdrawing groups on the ortho position of the anilide increased potency 20-40-fold and could be of utility to ameliorate conditions of inappropriate blood lactate elevation.

TL;DR: The oxime 12 and dehydroabietyl amine 2 exhibit a blood glucose lowering effect in the diabetic ob/ob mouse after a single oral dose of 100 micromol/kg, however, the mechanism of the blood glucose lowered effect is likely unrelated to PDK inhibition.

TL;DR: This article showed that triterpenes with 17-β hydroxyl and abietane derivatives are inhibitors of pyruvate dehydrogenase kinase (PDK) activity.