Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 16, Pages 4044-4047Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.05.072
Keywords
Vanilloid receptor 1; TRPV1 antagonist; Capsaicin; Resiniferatoxin; Molecular modeling
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Funding
- Research Grants from Grunenthal, Germany
- National Research Foundation of Korea (NRF) [R11-2007-107-02001-0]
- National Leading Research Lab (NLRL) program, Republic of Korea [2011-0028885]
- Intramural Research Program of NIH, Center for Cancer Research, NCI, USA [Z1A BC 005270]
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A series of 2-aryl pyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Multiple compounds showed highly potent TRPV1 antagonism toward capsaicin comparable to previous lead 7. Among them, compound 9 demonstrated anti-allodynia in a mouse neuropathic pain model and blocked capsaicin-induced hypothermia in a dose-dependent manner. Docking analysis of 9 with our hTRPV1 homology model provided insight into its specific binding mode. (C) 2014 Elsevier Ltd. All rights reserved.
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