DSpace at EWHA: α-Substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists

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α-Substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists

Title: α-Substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists

Authors: Chung J.-U.; Kim S.Y.; Lim J.-O.; Choi H.-K.; Kang S.-U.; Yoon H.-S.; Ryu H.; Kang D.W.; Lee J.; Kang B.; Choi S.; Toth A.; Pearce L.V.; Pavlyukovets V.A.; Lundberg D.J.; Blumberg P.M.

Citation: Bioorganic and Medicinal Chemistry vol. 15, no. 18, pp. 6043 - 6053

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, K i = 41 and 39.2 nM and K i(ant) = 4.5 and 37 nM). © 2007.