N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands.

Abstract A series of N -4-methansulfonamidobenzyl- N ′-2-substituted-4- tert -butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG neurons. Their structure–activity relationship reveals that there is a space for another hydrophobic binding interaction around 2-position in 4- tert -butylbenzyl region. Among the prepared derivatives, 6n show the highest antagonistic activity against the vanilloid receptor (IC 50 =15 nM).