- Synthesis and evaluation of naphthoic acid derivatives as fluorescent probes to screen advanced glycation end-products breakers
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Advanced glycation end-products, namely AGEs, are involved in the pathogenesis of numerous diseases. If AGEs inhibitors are well-known, only few products are described as compounds able to destroy those deleterious products. In this work, we describe naphthoic acid derivatives, particularly 1-(naphthalen-1-yl)propane-1,2-dione 9, allowing the simple and rapid detection of AGEs breakers using a 96-well microplate fluorescence assay. Since the inaugurate publication about AGEs breakers whose activity was demonstrated using HPLC analysis, this work proposes the first assay suitable for automated and high throughput screening of AGEs breakers.
- Séro, Luc,Calard, Fran?ois,Sanguinet, Lionel,Levillain, Eric,Richomme, Pascal,Séraphin, Denis,Derbré, Séverine
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supporting information
p. 6716 - 6720
(2013/01/14)
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- Methods of Treating or Preventing Cardiac Disease Associated With a High Fat Diet
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The present invention relates to a method of treating or preventing cardiac disorders, myocardial inflammation or myocardial oxidative stress associated with a high fat diet or in a patient subjected to a high fat diet using the thiazolium compounds and compositions of the invention. The present invention also relates to a method of ameliorating weight gain, myocardial AGE accumulation associated, mitochondrial superoxide production, RAGE expression or PPARα expression with a high fat diet or in a patient subjected to a high fat diet using the thiazolium compounds and compositions of the invention.
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- Method and composition for rejuvenating hair, nails, tissues, cells and organs by ex-vivo or immersive treatment
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A method and composition for the treatment of hair, nail, ex-vivo organ, ex-vivo cell or ex-vivo tissue to improve the biomechanical and diffusional characteristics comprising an effective amount of a compound selected from the group consisting of compounds of the formula
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- Method for treating fibrotic diseases or other indications IC
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Provided, among other things, is a method of treating or ameliorating or preventing an indication of the invention in an animal, including a human comprising administering an effective amount of a compound of the formula I:
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- Preventing and reversing the formation of advanced glycosylation endproducts
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The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain agents useful are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.
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- Preventing and reversing advanced glycosylation endproducts
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The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises a thiazolium compound capable of inhibiting, and to some extent reversing, the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.
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- Synthesis and Nitration of Some Thieno-fused Analogues of the Benzo[a]quinolizinium Cation
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Three thieno-fused analogues of benzo[a]quinolizinium (1), thieno[3,2-a]- and thieno[2,3-a]quinolizinimn 4 and 5 and thiazolo[2,3-a]isoquinolinium (6), were synthesized by photocyclization of 1-(2-thienylvinyl)pyridinium salts 9a and 9b and 3-styrylthiazolium salt 9c, respectively. The nitration of the compounds 4, 5, and 6 occurred predominantly at positions 2, 3, and 7, respectively, while the nitro group was introduced into the 8- and 10-positions of 1 in the ratio of 68:32. The nmr and uv spectral properties and reduction potentials of 4-6 were also compared with those of the parent compound 1.
- Sato, Kiyoshi,Arai, Sadao,Yamagishi, Takamichi
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