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Issue 11, 2016
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The discovery of a potent series of carboxamide TRPA1 antagonists

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Abstract

A series of potent and selective carboxamide TRPA1 antagonists were identified by a high throughput screen. Structure–activity relationship studies around this series are described, resulting in a highly potent example of the series. Pharmacokinetic and skin flux data are presented for this compound. Efficacy was observed in a topical cinnamaldehyde flare study, providing a topical proof of pharmacology for this mechanism. These data suggest TRPA1 antagonism could be a viable mechanism to treat topical conditions such as atopic dermatitis.

Graphical abstract: The discovery of a potent series of carboxamide TRPA1 antagonists

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Supplementary files

Article information


Submitted
13 Jul 2016
Accepted
17 Aug 2016
First published
30 Aug 2016

Med. Chem. Commun., 2016,7, 2145-2158
Article type
Research Article

The discovery of a potent series of carboxamide TRPA1 antagonists

D. C. Pryde, B. Marron, C. G. West, S. Reister, G. Amato, K. Yoger, K. Padilla, J. Turner, N. A. Swain, P. J. Cox, S. E. Skerratt, T. Ryckmans, D. C. Blakemore, J. Warmus and A. C. Gerlach, Med. Chem. Commun., 2016, 7, 2145
DOI: 10.1039/C6MD00387G

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