N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino) benzyl] thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid …

…, J Lee, M Kang, M Shin, JM Kim, SU Kang…

Index: Lee, Jeewoo; Lee, Jiyoun; Kang, Myungshim; Shin, Myoungyoup; Kim, Ji-Min; Kang, Sang-Uk; Lim, Ju-Ok; Choi, Hyun-Kyung; Suh, Young-Ger; Park, Hyeung-Geun; Oh, Uhtaek; Kim, Hee-Doo; Park, Young-Ho; Ha, Hee-Jin; Kim, Young-Ho; Toth, Attila; Wang, Yun; Tran, Richard; Pearce, Larry V.; Lundberg, Daniel J.; Blumberg, Peter M. Journal of Medicinal Chemistry, 2003 , vol. 46, # 14 p. 3116 - 3126

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Citation Number: 122

Abstract

Isosteric replacement of the phenolic hydroxyl group in potent vanilloid receptor (VR1) agonists with the alkylsulfonamido group provides a series of compounds which are effective antagonists to the action of the capsaicin on rat VR1 heterologously expressed in Chinese hamster ovary (CHO) cells. In particular, compound 61, N-[2-(3, 4-dimethylbenzyl)- 3-pivaloyloxypropyl]-N'-[3-fluoro-4-(methylsulfonylamino) benzyl] thiourea was a full ...