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• W2043150186 abstract "A series of potent antagonists of the ion channel transient receptor potential A1 (TRPA1) was developed by modifying lead structure 16 that was discovered by high-throughput screening. Based on lead compound 16, a SAR was established, showing a narrow region at the nitro-aromatic R1 moiety and at the warhead, while the R2 side had a much wider scope including ureas and carbamates. Compound 16 inhibits Ca2+-activated TRPA1 currents reversibly in whole cell patch clamp experiments, indicating that under in vivo conditions, it does not react covalently, despite its potentially electrophilic ketone." @default.
• W2043150186 created "2016-06-24" @default.
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• W2043150186 date "2012-09-01" @default.
• W2043150186 modified "2023-09-24" @default.
• W2043150186 title "N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor" @default.
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• W2043150186 doi "https://doi.org/10.1016/j.bmcl.2012.07.032" @default.
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