Synthesis of N,N',N"-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor

Bioorg Med Chem Lett. 2003 Feb 24;13(4):601-4. doi: 10.1016/s0960-894x(02)01040-5.

Abstract

Twenty-seven N,N',N"-trisubstituted thiourea derivatives were prepared. Among them, 1-[3-(4'-hydroxy-3'-methoxy-phenyl)-propyl]-1,3-diphenethyl-thiourea (8l, IC(50)=0.32 microM), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC(50)=0.65 microM) against the vanilloid receptor in a (45)Ca(2+)-influx assay.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Animals, Newborn
  • Calcium / metabolism
  • Calcium Isotopes
  • Capsaicin / analogs & derivatives
  • Inhibitory Concentration 50
  • Ion Channels / antagonists & inhibitors
  • Neurons / cytology
  • Neurons / drug effects
  • Neurons / physiology
  • Rats
  • Receptors, Drug / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Thiourea / chemical synthesis*
  • Thiourea / pharmacology

Substances

  • Calcium Isotopes
  • Ion Channels
  • Receptors, Drug
  • Thiourea
  • Capsaicin
  • Calcium