17623-72-2Relevant academic research and scientific papers
BENZAMIDE TRPA1 ANTAGONISTS
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Page/Page column 35, (2014/12/12)
Compounds of formula I, pharmaceutically acceptable salts thereof, diastereomers, enantiomers, or mixtures thereof: wherein R, X, Y, Z, n and A are as defined in the specification, as well as pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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
supporting information; experimental part, 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.
Diastereochemical diversity of imidazoline scaffolds via substrate controlled TMSCI mediated cycloaddition of azlactones
Sharma, Vasudha,Tepe, Jetze J.
, p. 5091 - 5094 (2007/10/03)
(Chemical Equation Presented) We report herein a trimethylsilyl chloride mediated substrate controlled 1,3-dipolar cycloaddition for the diastereoselective synthesis of either syn- or anti-imidazolines. This method provides scaffolds with four points of diversity and control over two stereocenters.
Intramolecular Participation by a Neighboring Amide Group in the Hydrolysis of N-Acylimidazoles
Kogan, Robert L.,Fife, Thomas H.
, p. 5229 - 5232 (2007/10/02)
Rate constants have been determined for the disappearance of the N-acylimidazole derivatives of N-acetylphenylalanine and N-acetylvaline in H2O at 30 deg C.The pH-rate constant profiles are characterized by large pH-independent regions.These reactions are
