Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1751-5. doi: 10.1016/j.bmcl.2004.01.066.

Abstract

A series of chain-branched 1,3-dibenzylthiourea derivatives were synthesized, and tested their antagonist activity against vanilloid receptor 1. Chain-branching led to a significant change in the mode of action and the potency. (R)-Methyl or ethyl-branched 1,3-dibenzylthiourea derivatives showed the most potent antagonist activity up to the IC(50) value of 0.05 microM which is 10-fold more potent than capsazepine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cells, Cultured
  • Neurons, Afferent / drug effects
  • Neurons, Afferent / metabolism
  • Rats
  • Receptors, Drug / antagonists & inhibitors*
  • Receptors, Drug / metabolism
  • Thiourea / chemistry*
  • Thiourea / metabolism
  • Thiourea / pharmacology

Substances

  • Receptors, Drug
  • Thiourea