203065-56-9Relevant academic research and scientific papers
Fluorescent probe for detecting activity of hydrogen peroxide, preparation and application
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Paragraph 0039, (2018/01/03)
The invention provides a fluorescent probe for detecting the activity of hydrogen peroxide. The fluorescent probe is obtained by the following steps: dissolving aspirin in dichloromethane, adding 1-hydroxybenzotriazole, 1-ethyl-(3-dimethylaminopropyl) car
ANTI-INFLAMMATORY COMPOUNDS AND USES THEREOF
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Page/Page column 43; 44, (2009/04/25)
Compounds of the general Formula (I) are disclosed with activity towards treating diseases related to inflammation, such as cancer, neurodegenerative and cardiovascular diseases. Pharmaceutical compositions and methods of use are also described.
Chemical insights in the concept of hybrid drugs: The antitumor effect of nitric oxide-donating aspirin involves a quinone methide but not nitric oxide nor aspirin
Hulsman, Niels,Medema, Jan Paul,Bos, Carina,Jongejan, Aldo,Leurs, Rob,Smit, Martine J.,De Esch, Iwan J. P.,Richel, Dick,Wijtmans, Maikel
, p. 2424 - 2431 (2008/02/03)
Hybrid drug 1 (NO-ASA) continues to attract intense research from chemists and biologists alike. It consists of ASA and a -ONO2 group connected through a spacer and is in preclinical development as an antitumor drug. We report that, contrary to current beliefs, neither ASA nor NO contributes to this antitumor effect. Rather, an unsubstituted QM was identified as the sole cytotoxic agent. QM forms from 1 after carboxylic ester hydrolysis and, in accordance with the HSAB theory, selectively reacts with cellular GSH, which in turn triggers cell death. Remarkably, a derivative lacking ASA and the -ONO 2 group is 10 times more effective than 1. Thus, our data provide a conclusive molecular mechanism for the antitumor activity of 1. Equally importantly, we show for the first time that a "presumed invisible" linker in a hybrid drug is not so invisible after all and is in fact solely responsible for the biological effect.
HIV-1 integrase inhibition of biscoumarin analogues
Chang-Xiao,Mouscadet, Jean-Francois,Chiang, Chih-Chia,Tsai, Hou-Jen,Hsu, Ling-Yih
, p. 682 - 686 (2007/10/03)
Nineteen biscoumarins bearing free and modified hydroxyl substituents at benzoyloxyphenyl linker have been synthesized by multiple step synthesis. Among these biscoumarins, thirteen were found to be active molecules against HIV-1 integrase (HIV-1 IN). The structure-activity relationship of the nineteen compounds on HIV IN may be useful for the design of potent therapeutic agents.
Drugs for diabetes
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, (2008/06/13)
Use for the diabetes treatment of compounds or salts thereof, having the following general formula (I): A-(B)b0—(C)c0—NO2 wherein A contains the radical of a drug having an antiiflammatory or analgesic activity, B is a bivalen: linking group wherein the precursor must meet the tests described in the application, C is a a bivalent linking group as defined in the invention.
Nitroderivatives as drugs for diseases having an inflammatory basis
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, (2008/06/13)
Use for the treatment of diseases having an inflammatory basis of compounds or salts thereof, having the following general formula (I): A-Xt-L-(W)p—NO2 wherein A contains the radical of a drug, Xt and W arc bivalent radicals, L, is a covalent bond or oxygen, sulphur, NRtc wherein Rtc is H or a C1-C5 linear or branched alkyl.
Nitric oxide-donating non-steroidal anti-inflammatory drugs: The case of nitroderivatives of aspirin
Chiroli, Valerio,Benedini, Francesca,Ongini, Ennio,Del Soldato, Piero
, p. 441 - 446 (2007/10/03)
Nitric oxide (NO) acts as a key signalling mechanism in a number of cells and tissues in the mammalian organism. Modulation of the biosynthesis of NO has emerged to be relevant to the treatment of a variety of human diseases. In the attempt to reduce the serious side effects of non-steroidal anti-inflammatory drugs (NSAIDs), especially in the gastrointestinal tract, a NO-releasing moiety has been linked to conventional NSAIDs. A prototypical example is that of NO-releasing derivatives of aspirin. Thanks to the cytoprotective action of NO such compounds do not produce gastric damage and are emerging as an interesting novel group of drugs for their unique pharmacological properties.
Prodrugs - Part 1. Formylphenyl esters of aspirin
Bowden,Huntington,Powell
, p. 987 - 993 (2007/10/03)
The synthesis and study of a novel series of potential prodrugs of aspirin is reported. 2-, 3- and 4-formylphenyl aspirins, as well as a series of 4-substituted 2-formylphenyl aspirins, have been prepared. A study of their alkaline hydrolysis indicates that these compounds act as true prodrugs of aspirin which hydrolyse to aspirin and the formylphenol. The rates of hydrolysis and activation parameters indicate that hydrolysis of the 2-formylphenyl esters employs an intramolecular catalytic route.
