Title of article
α-Substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists Original Research Article
Author/Authors
Jae-Uk Chung، نويسنده , , Su Yeon Kim ، نويسنده , , Ju-Ok Lim، نويسنده , , Hyun-Kyung Choi، نويسنده , , Sang Uk Kang، نويسنده , , Hae-Seok Yoon، نويسنده , , HyungChul Ryu، نويسنده , , Dong Wook Kang، نويسنده , , Jeewoo Lee، نويسنده , , Bomi Kang، نويسنده , , Sun Choi، نويسنده , , Attila Toth، نويسنده , , Larry V. Pearce، نويسنده , , Vladimir A. Pavlyukovets، نويسنده , , Daniel J. Lundberg، نويسنده , , Peter M. Blumberg، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
11
From page
6043
To page
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, Ki = 41 and 39.2 nM and Ki(ant) = 4.5 and 37 nM).
Keywords
TRPV1 antagonists , Analgesic
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2007
Journal title
Bioorganic and Medicinal Chemistry
Record number
1305988
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