TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides

Tae Hwan Ha, Hyungchul Ryu, Sung Eun Kim, Ho Shin Kim, Jihyae Ann, Phuong Thao Tran, Van Hai Hoang, Karam Son, Minghua Cui, Sun Choi, Peter M. Blumberg, Robert Frank, Gregor Bahrenberg, Klaus Schiene, Thomas Christoph, Sven Frormann, Jeewoo Lee

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21 Scopus citations


A series of 2-thio pyridine C-region analogues of 2-(3-fluoro-4- methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. Among them, compound 24S showed stereospecific and excellent TRPV1 antagonism of capsaicin-induced activation. Further, it demonstrated strong anti-allodynic in a rat neuropathic pain model. Consistent with its action in vitro being through TRPV1, compound 24S blocked capsaicin-induced hypothermia in mice. Docking analysis of 24S with our hTRPV1 homology model was performed to identify its binding mode.

Original languageEnglish
Pages (from-to)6657-6664
Number of pages8
JournalBioorganic and Medicinal Chemistry
Issue number21
StatePublished - 1 Nov 2013

Bibliographical note

Funding Information:
This research was supported by Research Grants from Grunenthal, Grants from the National Research Foundation of Korea (NRF) ( R11-2007-107-02001-0 ), Grants from the National Leading Research Lab (NLRL) program ( 2011-0028885 ), and in part by the Intramural Research Program of NIH, Center for Cancer Research, NCI (Project Z1A BC 005270 ).


  • Analgesic
  • Capsaicin
  • Resiniferatoxin
  • TRPV1 antagonists


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