Medicinal chemistry, pharmacology, and clinical implications of TRPV1 receptor antagonists
M Aghazadeh Tabrizi, PG Baraldi… - Medicinal research …, 2017 - Wiley Online Library
Transient receptor potential vanilloid 1 (TRPV1) is an ion channel expressed on sensory
neurons triggering an influx of cations. TRPV1 receptors function as homotetramers …
neurons triggering an influx of cations. TRPV1 receptors function as homotetramers …
Modulation of the TRPV1 channel: current clinical trials and recent patents with focus on neurological conditions
L De Petrocellis, AS Moriello - Recent Patents on CNS Drug …, 2013 - ingentaconnect.com
The transient receptor potential vanilloid-1 cat ion channel (TRPV1) is a nonspecific cation
channel that can be activated by multiple endogenous stimuli and is expressed …
channel that can be activated by multiple endogenous stimuli and is expressed …
Structural insight into tetrameric hTRPV1 from homology modeling, molecular docking, molecular dynamics simulation, virtual screening, and bioassay validations
The transient receptor potential vanilloid type 1 (TRPV1) is a heat-activated cation channel
protein, which contributes to inflammation, acute and persistent pain. Antagonists of human …
protein, which contributes to inflammation, acute and persistent pain. Antagonists of human …
Pyrazole C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl) propanamides as potent TRPV1 antagonists
S Lee, C Kim, J Ann, SA Thorat, E Kim, J Park… - Bioorganic & medicinal …, 2017 - Elsevier
Abstract A series of 1-substituted 3-(t-butyl/trifluoromethyl) pyrazole C-region analogues of 2-
(3-fluoro-4-methylsulfonamidophenyl) propanamides were investigated for h TRPV1 …
(3-fluoro-4-methylsulfonamidophenyl) propanamides were investigated for h TRPV1 …
Discovery of indane propanamides as potent and selective TRPV1 antagonists
A series of indane-type acetamide and propanamide analogues were investigated as
TRPV1 antagonists. The analysis of structure–activity relationship indicated that indane A …
TRPV1 antagonists. The analysis of structure–activity relationship indicated that indane A …
TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl) propanamides
A series of 2-thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)
propanamides were investigated as h TRPV1 antagonists. Among them, compound 24S …
propanamides were investigated as h TRPV1 antagonists. Among them, compound 24S …
2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl) propanamides as highly potent TRPV1 antagonists
HC Ryu, S Seo, SH Cho, HS Kim, A Jung… - Bioorganic & medicinal …, 2014 - Elsevier
A series of 2-alkyl/alkenyl pyridine C-region derivatives of 2-(3-fluoro-4-
methylsulfonylaminophenyl) propanamides were investigated as h TRPV1 antagonists …
methylsulfonylaminophenyl) propanamides were investigated as h TRPV1 antagonists …
Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl) propanamides as potent TRPV1 antagonists
HC Ryu, S Seo, JY Lee, TH Ha, S Lee, A Jung… - European journal of …, 2015 - Elsevier
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 h TRPV1 …
(3-fluoro-4-methylsulfonylaminophenyl) propanamides were investigated as h TRPV1 …
[PDF][PDF] Directed lithiation and substitution of pyridine derivatives
GA El-Hiti, K Smith, AS Hegazy - Heterocycles, 2015 - triggered.edinburgh.clockss.org
Directed lithiation of substituted pyridines containing a directing metalating group (DMG)
with a lithium reagent in anhydrous solvent at low temperature gives the corresponding …
with a lithium reagent in anhydrous solvent at low temperature gives the corresponding …
2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl) propanamides as highly potent TRPV1 antagonists
A series of 2-aryl pyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonylaminophenyl)
propanamides were investigated as h TRPV1 antagonists. Multiple compounds showed …
propanamides were investigated as h TRPV1 antagonists. Multiple compounds showed …