Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agents

Bioorg Med Chem Lett. 2006 Jan 1;16(1):113-7. doi: 10.1016/j.bmcl.2005.09.034. Epub 2005 Oct 10.

Abstract

A series of 1-alkyl-3-phenylthiourea analogues were prepared and evaluated as HDL- and Apo A-I-elevating and triglyceride-lowering agents. Several derivatives were superior to gemfibrozil. The optimal analogue (HDL376) was shown to raise HDL cholesterol in the rat, hamster, dog, and monkey models.

MeSH terms

  • Administration, Oral
  • Animals
  • Centrifugation, Density Gradient
  • Cholesterol, HDL / metabolism
  • Chromatography, High Pressure Liquid
  • Cricetinae
  • Dogs
  • Drug Evaluation, Preclinical
  • Gemfibrozil / pharmacology*
  • Haplorhini
  • Lipids / chemistry
  • Lipoproteins, HDL / metabolism*
  • Male
  • Models, Chemical
  • Phenylthiourea / administration & dosage
  • Phenylthiourea / chemical synthesis*
  • Phenylthiourea / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Time Factors
  • Triglycerides / metabolism

Substances

  • Cholesterol, HDL
  • Lipids
  • Lipoproteins, HDL
  • Triglycerides
  • Phenylthiourea
  • Gemfibrozil