@article{25dc280d193e415280231304fb2cb2e5,
title = "α-Substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists",
abstract = "A series of α-substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. α-Methyl substituted analogues showed potent and stereospecific antagonism to the action of capsaicin on rat TRPV1 heterologously expressed in Chinese hamster ovary cells. In particular, compounds 14 and 18, which possess the R-configuration, exhibited excellent potencies (respectively, Ki = 41 and 39.2 nM and Ki(ant) = 4.5 and 37 nM).",
keywords = "Analgesic, TRPV1 antagonists",
author = "Chung, {Jae Uk} and Kim, {Su Yeon} and Lim, {Ju Ok} and Choi, {Hyun Kyung} and Kang, {Sang Uk} and Yoon, {Hae Seok} and Ryu, {Hyung Chul} and Kang, {Dong Wook} and Jeewoo Lee and Bomi Kang and Sun Choi and Attila Toth and Pearce, {Larry V.} and Pavlyukovets, {Vladimir A.} and Lundberg, {Daniel J.} and Blumberg, {Peter M.}",
note = "Funding Information: This work was supported by Grant R01-2004-000-10132-0 from the Basic Research Program of the Korea Science & Engineering Foundation and by Grant No. R15-2006-020 from the National Core Research Center (NCRC) program of the Ministry of Science & Technology (MOST) through the Center for Cell Signaling & Drug Discovery Research at Ewha Womans University. This work was also supported in part by the Intramural Research Program of the NIH, National Cancer Institute, Center for Cancer Research. We thank Richard Tran and Matthew A. Morgan for technical assistance.",
year = "2007",
month = sep,
day = "15",
doi = "10.1016/j.bmc.2007.06.041",
language = "English",
volume = "15",
pages = "6043--6053",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Ltd.",
number = "18",
}