Details

Autor(en) / Beteiligte

• Ryu, HyungChul
• Seo, Sejin
• Lee, Jee-Young
• Ha, Tae-Hwan
• Lee, Sunho
• Jung, Aeran
• Ann, Jihyae
• Kim, Sung-Eun
• Yoon, Suyoung
• Hong, Mannkyu
• Blumberg, Peter M.
• Frank-Foltyn, Robert
• Bahrenberg, Gregor
• Schiene, Klaus
• Stockhausen, Hannelore
• Christoph, Thomas
• Frormann, Sven
• Lee, Jeewoo

Titel

Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists

Ist Teil von

• European journal of medicinal chemistry, 2015-03, Vol.93, p.101-108

Ort / Verlag

France: Elsevier Masson SAS

Erscheinungsjahr

2015

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• A series of pyridine derivatives in the C-region of N-((6-trifluoromethyl-pyridin-3-yl)methyl) 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists. The SAR analysis indicated that 6-difluorochloromethyl pyridine derivatives were the best surrogates of the C-region for previous leads. Among them, compound 31 showed excellent antagonism to capsaicin as well as to multiple hTRPV1 activators. It demonstrated strong analgesic activity in the formalin test in mice with full efficacy and it blocked capsaicin-induced hypothermia in vivo. [Display omitted] •A series of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides were investigated as hTRPV1 antagonists.•Compound 31 showed potent antagonisms toward hTRPV1 multiple activators.•Compound 31 exhibited strong analgesic activity.