82129-08-6Relevant academic research and scientific papers
1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase
Keith, John M.,Hawryluk, Natalie,Apodaca, Richard L.,Chambers, Allison,Pierce, Joan M.,Seierstad, Mark,Palmer, James A.,Webb, Michael,Karbarz, Mark J.,Scott, Brian P.,Wilson, Sandy J.,Luo, Lin,Wennerholm, Michelle L.,Chang, Leon,Rizzolio, Michele,Chaplan, Sandra R.,Breitenbucher, J. Guy
, p. 1280 - 1284 (2014/03/21)
A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was efficacious in a rat model of neuropathic pain.
Cyanosilylation of aldehydes and ketones catalyzed by nanocrystalline magnesium oxide
Lakshmi Kantam,Mahendar, Koosam,Sreedhar, Bojja,Vijay Kumar,Choudary
experimental part, p. 3919 - 3936 (2009/04/11)
Cyanosilylation of various aldehydes and ketones with TMSCN proceeded smoothly under mild conditions to give the corresponding cyanohydrin trimethylsilyl ethers in the presence of nanocrystalline magnesium oxide. The cyanohydrin trimethylsilyl ethers of aldehydes produced cyanohydrins in good to high yields on treatment with 2 N HCl. 29Si NMR spectral evidence proved that the reaction proceeds through the hypervalent silicate species by coordination to O2-/O- (Lewis basic site) of nanocrystalline magnesium oxide. Copyright Taylor & Francis Group, LLC.
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
Jarvest, Richard L.,Erskine, Symon G.,Forrest, Andrew K.,Fosberry, Andrew P.,Hibbs, Martin J.,Jones, Joanna J.,O'Hanlon, Peter J.,Sheppard, Robert J.,Worby, Angela
, p. 2305 - 2309 (2007/10/03)
High throughput screening of Staphylococcus aureus phenylalanyl tRNA synthetase (FRS) identified ethanolamine 1 as a sub-micromolar hit. Optimisation studies led to the enantiospecific lead 64, a single-figure nanomolar inhibitor. The inhibitor series shows selectivity with respect to the mammalian enzyme and the potential for broad spectrum bacterial FRS inhibition.
Hypoglycemic 5-substituted oxazolidine-2,4-diones
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, (2008/06/13)
Hypoglycemic 5-phenyl and 5-naphthyl oxazolidine-2,4-diones and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.
