1. Academic Validation
  2. Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK)

Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK)

  • Bioorg Med Chem Lett. 1999 Aug 2;9(15):2223-8. doi: 10.1016/s0960-894x(99)00380-7.
T D Aicher 1 R E Damon J Koletar C C Vinluan L J Brand J Gao S S Shetty E L Kaplan W R Mann
Affiliations

Affiliation

  • 1 Metabolic & Cardiovascular Diesases Research, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA.
Abstract

Several oximes of Triterpenes with a 17-beta hydroxyl and abietane derivatives are inhibitors of pyruvate dehydrogenase kinase (PDK) activity. 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 lowering effect is likely unrelated to PDK inhibition.

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