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

YG Suh, YS Lee, KH Min, OH Park, JK Kim…

Index: Suh, Young-Ger; Lee, Yong-Sil; Min, Kyung-Hoon; Park, Ok-Hui; Kim, Jin-Kwan; Seung, Ho-Sun; Seo, Seung-Yong; Lee, Bo-Young; Nam, Yeon-Hee; Lee, Kwang-Ok; Kim, Hee-Doo; Park, Hyeung-Geun; Lee, Jeewoo; Oh, Uhtaek; Lim, Ju-Ok; Kang, Sang-Uk; Kil, Min-Jung; Koo, Jae-Yeon; Shin, Song Seok; Joo, Yung-Hyup; Kim, Jin Kwan; Jeong, Yeon-Su; Kim, Sun-Young; Park, Young-Ho Journal of Medicinal Chemistry, 2005 , vol. 48, # 18 p. 5823 - 5836

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Citation Number: 45

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, ...