2. Academic Validation
  3. Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents

Novel potent antagonists of transient receptor potential channel, vanilloid subfamily member 1: structure-activity relationship of 1,3-diarylalkyl thioureas possessing new vanilloid equivalents

  • J Med Chem. 2005 Sep 8;48(18):5823-36. doi: 10.1021/jm0502790.
Young-Ger Suh 1,  Yong-Sil Lee,  Kyung-Hoon Min,  Ok-Hui Park,  Jin-Kwan Kim,  Ho-Sun Seung,  Seung-Yong Seo,  Bo-Young Lee,  Yeon-Hee Nam,  Kwang-Ok Lee,  Hee-Doo Kim,  Hyeung-Geun Park,  Jeewoo Lee,  Uhtaek Oh,  Ju-Ok Lim,  Sang-Uk Kang,  Min-Jung Kil,  Jae-Yeon Koo,  Song Seok Shin,  Yung-Hyup Joo,  Jin Kwan Kim,  Yeon-Su Jeong,  Sun-Young Kim,  Young-Ho Park
Affiliations

Affiliation

  • 1 College of Pharmacy, and Sensory Research Center, CRI, Seoul National University, San 56-1, Shinlim-Dong, Kwanak-Gu, Seoul 151-742, Korea. [email protected]
PMID: 16134949 DOI: 10.1021/jm0502790
Abstract

Recently, 1,3-diarylalkyl thioureas have merged as one of the promising nonvanilloid TRPV1 antagonists possessing excellent therapeutic potential in pain regulation. In this paper, the full structure-activity relationship for TRPV1 antagonism of a novel series of 1,3-diarylalky thioureas is reported. Exploration of the structure-activity relationship, by systemically modulating three essential pharmacophoric regions, led to six examples of 1,3-dibenzyl thioureas, which exhibit CA(2+) uptake inhibition in rat DRG neuron with IC(50) between 10 and 100 nM.

Figures