113535-07-2Relevant academic research and scientific papers
N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor
Vallin, Karl S.A.,Sterky, Karin J.,Nyman, Eva,Bernstroem, Jenny,From, Rebecka,Linde, Christian,Minidis, Alexander B.E.,Nolting, Andreas,Naerhi, Katja,Santangelo, Ellen M.,Sehgelmeble, Fernando W.,Sohn, Daniel,Strindlund, Jennie,Weigelt, Dirk
, p. 5485 - 5492 (2012/09/22)
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.
Aminoketone, oxazole and thiazole synthesis. Part XIII. 1 new 2-aryl-6-phenyloxazoles with 4-methyl or 4-isopropyl groups
Schiketanz, Iosif,Istrati, Daniela,Drǎghici, Constantin,Balaban, Alexandru T.
, p. 137 - 142 (2007/10/03)
Benzoylation of (±)-α-alanine and (±)-valine followed by cyclization afforded the corresponding azlactones, which reacted with benzene, toluene, o- and m-xylene yielding substituted N-benzoyl-phenacylamines. Their cyclization in the presence of phosphorus oxychloride led to the title compounds whose electronic and NMR spectra (1H and 13C) are presented.
