Synthesis and the antiperoxidase activity of seleno analogues of the antithyroid drug propylthiouracil

J Enzyme Inhib. 1993;7(2):147-50. doi: 10.3109/14756369309040756.

Abstract

The synthesis of 6-n-propyl-2-selenouracil (PSeU, Ib) and its methyl derivative (MSeU, Ic) are described. Replacement of the sulfur atom at C2 by selenium increased with antiperoxidase activity of these analogues five fold when compared to the clinically used antithyroid drug propylthiouracil (PTU). The structure-activity relationships of these agents are discussed.

MeSH terms

  • Animals
  • Peroxidases / antagonists & inhibitors*
  • Propylthiouracil / analogs & derivatives*
  • Propylthiouracil / pharmacology
  • Selenium Compounds / chemical synthesis*
  • Selenium Compounds / pharmacology
  • Structure-Activity Relationship
  • Swine
  • Thyroid Gland / drug effects
  • Thyroid Gland / enzymology

Substances

  • Selenium Compounds
  • Propylthiouracil
  • Peroxidases