Novel Potent Antagonists of Transient Receptor Potential Channel, Vanilloid Subfamily Member 1: Structure−Activity Relationship of 1,3-Diarylalkyl Thioureas Possessing New Vanilloid Equivalents
Journal of Medicinal Chemistry2005Vol. 48(18), pp. 5823–5836
Citations Over Time
Young‐Ger Suh, Yong‐Sil Lee, Kyung‐Hoon Min, Ok-Hui Park, Jin-Kwan Kim, Ho-Sun Seung, Seung‐Yong Seo, Boyoung 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, Jaeyeon Koo, Song Seok Shin, Young Hoon Joo, Jin Kwan Kim, Yeonsu Jeong, Sunyoung Kim, Young‐Ho Park
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.
Related Papers
- → The Role of Transient Receptor Potential Vanilloid 1 in Common Diseases of the Digestive Tract and the Cardiovascular and Respiratory System(2019)123 cited
- TRP channel antagonists for pain--opportunities beyond TRPV1.(2009)
- → Unique Responses are Observed in Transient Receptor Potential Ankyrin 1 and Vanilloid 1 (TRPA1 and TRPV1) Co-Expressing Cells(2014)34 cited
- → Vanilloid (TRPV1) and Other Transient Receptor Potential Channels(2009)2 cited
- Role of transient receptor potential vanilloid 1 channel in pancreatitis(2009)