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Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2015 Mar 26; Vol. 93, pp. 101-8. Date of Electronic Publication: 2015 Feb 02. - Publication Year :
- 2015
-
Abstract
- 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.<br /> (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Analgesics chemistry
Analgesics pharmacology
Analgesics therapeutic use
Animals
Benzeneacetamides chemistry
Benzeneacetamides pharmacology
Benzeneacetamides therapeutic use
Mice
Molecular Structure
Pain drug therapy
Pain Measurement
Structure-Activity Relationship
Sulfonamides chemistry
Sulfonamides pharmacology
Sulfonamides therapeutic use
Analgesics chemical synthesis
Benzeneacetamides chemical synthesis
Pyridines chemistry
Sulfonamides chemical synthesis
TRPV Cation Channels antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 93
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 25659771
- Full Text :
- https://doi.org/10.1016/j.ejmech.2015.02.001