Discovery of piperidine carboxamide TRPV1 antagonists
A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential receptor 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 potenc...
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Published in | Bioorganic & medicinal chemistry Vol. 18; no. 16; pp. 4569 - 4572 |
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Main Authors | , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
15.08.2008
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential receptor 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.
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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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0960-894X 0968-0896 1464-3405 1464-3391 |
DOI: | 10.1016/j.bmcl.2008.07.035 |