Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4143-50. doi: 10.1016/j.bmcl.2005.06.006.

Abstract

The structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. A docking model of potent antagonist 2 with the sensor region of TRPV1 is proposed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Ligands
  • Models, Molecular
  • Protein Structure, Tertiary
  • Structure-Activity Relationship
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology*
  • TRPV Cation Channels / antagonists & inhibitors*
  • TRPV Cation Channels / chemistry
  • TRPV Cation Channels / metabolism
  • Thiocarbamates / chemical synthesis
  • Thiocarbamates / chemistry
  • Thiourea / analogs & derivatives*
  • Thiourea / chemistry
  • Thiourea / pharmacology*

Substances

  • Ligands
  • N-(4-t-butylbenzyl)-N'-(4-(methylsulfonylamino)benzyl)thiourea
  • Sulfonamides
  • TRPV Cation Channels
  • TRPV1 receptor
  • Thiocarbamates
  • Thiourea