694529-17-4Relevant articles and documents
α-Substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists
Chung, Jae-Uk,Kim, Su Yeon,Lim, Ju-Ok,Choi, Hyun-Kyung,Kang, Sang-Uk,Yoon, Hae-Seok,Ryu, HyungChul,Kang, Dong Wook,Lee, Jeewoo,Kang, Bomi,Choi, Sun,Toth, Attila,Pearce, Larry V.,Pavlyukovets, Vladimir A.,Lundberg, Daniel J.,Blumberg, Peter M.
, p. 6043 - 6053 (2008/03/18)
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).
Chain-branched 1,3-dibenzylthioureas as vanilloid receptor 1 antagonists
Ryu, Chong Hyun,Jang, Mi Jung,Jung, Jeong Wha,Park, Ju-Hyun,Choi, Hye Young,Suh, Young-Ger,Oh, Uhtaek,Park, Hyeung-Geun,Lee, Jeewoo,Koh, Hyun-Joo,Mo, Joo-Hyun,Joo, Yung Hyup,Park, Young-Ho,Kim, Hee-Doo
, p. 1751 - 1755 (2007/10/03)
A series of chain-branched 1,3-dibenzylthiourea derivatives were synthesized, and tested their antagonist activity against vanilloid receptor 1. Chain-branching led to a significant change in the mode of action and the potency. (R)-Methyl or ethyl-branched 1,3-dibenzylthiourea derivatives showed the most potent antagonist activity up to the IC50 value of 0.05 μM which is 10-fold more potent than capsazepine.
