81518-54-9Relevant academic research and scientific papers
NAPHTHYLACETIC ACIDS
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Page/Page column 87, (2010/06/15)
The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds of formula (I) are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
Inactivation of mitochondrial monoamine oxidase B by methylthio-substituted benzylamines
Lu, Xingliang,Rodriguez, Maria,Gu, Wenxin,Silverman, Richard B.
, p. 4423 - 4430 (2007/10/03)
Mitochondrial monoamine oxidase was inactivated by o-mercaptobenzylamine (1) and o- (2) and p-methylthiobenzylamine (5). Experiments were carried out to provide evidence for possible mechanisms of inactivation. The corresponding o- (3) and p-hydroxybenzylamine (4) are not inactivators. Four radiolabeled analogues of 2 and 5, having radioactivity at either the methyl or benzyl groups, were synthesized, and all were shown to incorporate multiple equivalents of radioactivity into the enzyme. Inactivation in the presence of an electrophile scavenger decreased the number of molecules incorporated, but still multiple molecules became incorporated; catalase did not further reduce the number of inactivator molecules bound. Two inactivation mechanisms are proposed, one involving a nucleophilic aromatic substitution (SNAr) mechanism and the other a dealkylation mechanism. Evidence for both mechanisms is that inactivation leads to reduction of the flavin (oxidation of the inactivator), but upon denaturation the flavin is reoxidized, indicating that attachment is not at the flavin. A cysteine titration indicates the loss of four cysteines after inactivation and denaturation. Support for the S NAr mechanism was obtained by showing that o- and p-chlorobenzylamine also inactivate MAO. Chemical model studies were carried out that also support both SNAr and dealkylation mechanisms.
Process for treating hyperglycemia using trifluoromethyl substituted 3H-pyrazol-3-ones
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, (2008/06/13)
The compound of the formula: STR1 in which the dotted lines represent two sites of unsaturation appropriately located based on the identity of R2, R3 and R4 and, R1 is alkyl, perfluoroalkyl, alkoxy, perfluoroalk
