Abstract |
A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential vanilloid-1 (TRPV1), an emerging target for the treatment of pain. A focused library of polar head groups led to the identification of a benzoxazinone amide that afforded good potency in cell-based assays. Synthesis and a QSAR model will be presented.
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Authors | Wing S Cheung, Raul R Calvo, Brett A Tounge, Sui-Po Zhang, Dennis R Stone, Michael R Brandt, Tasha Hutchinson, Christopher M Flores, Mark R Player |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 18
Issue 16
Pg. 4569-72
(Aug 15 2008)
ISSN: 1464-3405 [Electronic] England |
PMID | 18662879
(Publication Type: Journal Article)
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Chemical References |
- Amides
- Benzoxazines
- Carrier Proteins
- Piperidines
- TRPV Cation Channels
- TRPV1 protein, human
- Capsaicin
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Topics |
- Amides
(chemistry)
- Benzoxazines
(chemistry, pharmacology)
- Capsaicin
(chemistry)
- Carrier Proteins
(antagonists & inhibitors)
- Chemistry, Pharmaceutical
(methods)
- Drug Design
- Humans
- Inhibitory Concentration 50
- Models, Chemical
- Molecular Conformation
- Piperidines
(chemistry)
- Protein Binding
- Quantitative Structure-Activity Relationship
- Structure-Activity Relationship
- TRPV Cation Channels
(antagonists & inhibitors)
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