N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor

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 th...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-09, Vol.22 (17), p.5485-5492
Hauptverfasser:	Vallin, Karl S.A., Sterky, Karin J., Nyman, Eva, Bernström, Jenny, From, Rebecka, Linde, Christian, Minidis, Alexander B.E., Nolting, Andreas, Närhi, Katja, Santangelo, Ellen M., Sehgelmeble, Fernando W., Sohn, Daniel, Strindlund, Jennie, Weigelt, Dirk
Format:	Artikel
Sprache:	eng
Schlagworte:	amides Amides - chemistry Amides - pharmacology Antagonist Antagonists Biological and medical sciences Calcium - metabolism Calcium Channels - metabolism carbamates Carbamates - chemistry Carbamates - pharmacology chemistry high-throughput screening Humans Ion channel Ion channels ketones Lead Medical sciences Nerve Tissue Proteins - antagonists & inhibitors Nerve Tissue Proteins - metabolism Patch-Clamp Techniques Pharmacology. Drug treatments screening Structure-Activity Relationship Transient Receptor Potential Channels - antagonists & inhibitors Transient Receptor Potential Channels - metabolism transient receptor potential proteins TRPA1 TRPA1 Cation Channel Urea Urea - chemistry Urea - pharmacology
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