New barbiturates and thiobarbiturates as potential enzyme inhibitors

J Enzyme Inhib Med Chem. 2015 Feb;30(1):119-25. doi: 10.3109/14756366.2014.895717. Epub 2014 Mar 25.

Abstract

A series of 27 new barbiturates and thiobarbiturates have been synthesized by a convenient multi-component reaction in overall excellent yields (87-96%). All the synthesized compounds were characterized by 1H, 13C NMR, EIMS and elemental analysis (C, H, N and S). Furthermore, all compounds were screened for in vitro antioxidant (DPPH radical scavenging), lipoxygenase, chymotrypsin, α-glucosidase and anti-urease activities. Out of the series, 23 in DPPH, 14 in lipoxygenase, 2 in chymotrypsin have shown appreciable IC50 values.

Keywords: antioxidant (DPPH radical scavenging); barbituric acid; chymotrypsin; lipoxygenase; thiobarbituric acid; thiosemicarbazone; α-Glucosidase and anti-urease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antioxidants / chemical synthesis*
  • Antioxidants / chemistry
  • Barbiturates / chemical synthesis*
  • Barbiturates / chemistry
  • Biphenyl Compounds / antagonists & inhibitors
  • Chymotrypsin / antagonists & inhibitors
  • Chymotrypsin / chemistry
  • Enzyme Assays
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Lipoxygenase / chemistry
  • Picrates / antagonists & inhibitors
  • Thiobarbiturates / chemical synthesis*
  • Thiobarbiturates / chemistry
  • Urease / antagonists & inhibitors
  • Urease / chemistry
  • alpha-Glucosidases / chemistry

Substances

  • Antioxidants
  • Barbiturates
  • Biphenyl Compounds
  • Enzyme Inhibitors
  • Picrates
  • Thiobarbiturates
  • 1,1-diphenyl-2-picrylhydrazyl
  • Lipoxygenase
  • alpha-Glucosidases
  • Chymotrypsin
  • Urease