Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists

[Display omitted] A series of 2-substituted 4-(trifluoromethyl)benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides were investigated for hTRPV1 antagonism. The analysis indicated that the phenyl C-region derivatives exhibited better antagonism than those of the correspondin...

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Published in:	Bioorganic & medicinal chemistry 2015-11, Vol.23 (21), p.6844-6854
Main Authors:	Ann, Jihyae, Jung, Aeran, Kim, Mi-Yeon, Kim, Hyuk-Min, Ryu, HyungChul, Kim, Sunjoo, Kang, Dong Wook, Hong, Sunhye, Cui, Minghua, Choi, Sun, Blumberg, Peter M., Frank-Foltyn, Robert, Bahrenberg, Gregor, Stockhausen, Hannelore, Christoph, Thomas, Lee, Jeewoo
Format:	Article
Language:	English
Subjects:	Amides - chemical synthesis Amides - chemistry Amides - therapeutic use Analgesic Analgesics - chemical synthesis Analgesics - chemistry Animals Binding Sites Capsaicin - toxicity Humans Hypothermia - chemically induced Hypothermia - drug therapy Mice Molecular Conformation Molecular Docking Simulation Structure-Activity Relationship TRPV Cation Channels - antagonists & inhibitors TRPV Cation Channels - metabolism TRPV1 antagonists Vanilloid receptor 1
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