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
  • 1. Metabolic & Cardiovascular Diesases Research, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA.
PMID: 10465550 DOI: 10.1016/s0960-894x(99)00380-7
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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