- BENZAMIDE TRPA1 ANTAGONISTS
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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.
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Page/Page column 35
(2014/12/12)
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- N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor
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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.
- 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
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supporting information; experimental part
p. 5485 - 5492
(2012/09/22)
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- Diastereochemical diversity of imidazoline scaffolds via substrate controlled TMSCI mediated cycloaddition of azlactones
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(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.
- Sharma, Vasudha,Tepe, Jetze J.
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p. 5091 - 5094
(2007/10/03)
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- Intramolecular Participation by a Neighboring Amide Group in the Hydrolysis of N-Acylimidazoles
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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
- Kogan, Robert L.,Fife, Thomas H.
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p. 5229 - 5232
(2007/10/02)
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