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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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Publication details

The article was received on 13 Jul 2016, accepted on 17 Aug 2016 and first published on 30 Aug 2016


Article type: Research Article
DOI: 10.1039/C6MD00387G
Citation: Med. Chem. Commun., 2016,7, 2145-2158
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    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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