- Ibuprofen polymer prodrug and adriamycin co-assembled nano-particle and preparation method therefor
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The invention discloses an ibuprofen polymer prodrug and adriamycin co-assembled nano-particle and a preparation method therefor. According to the preparation method, a polymer prodrug having anti-inflammatory and anti-cancer combined action is obtained b
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Paragraph 0057-0062
(2020/07/24)
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- Organotin(IV) compounds derived from ibuprofen and cinnamic acids, an alternative into design of anti-inflammatory by the cyclooxygenases (COX-1 and COX-2) pathway
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New tributyl-, dibutyl- and diphenyl-tin(IV) complexes derived from ibuprofen and cinnamic acids were synthesized. All compounds were structurally characterized by FT-IR, multinuclear 1H, 13C, 19F and 119Sn NMR and corroborated by 2D spectra. The NMR data in CDCl3 revealed several hexacoordinated compounds with octahedral geometry. Moreover, in DMSO-d6 some of these complexes switched to heptacoordination with a pentagonal-bipyramidal geometry due to the inclusion of a solvent's molecule; their 119Sn signals moved up field by around 58 ppm compared to their chemical shifts in non-coordinated solvent CDCl3. The structural results were supported by Density Functional Theory (DFT) computational calculations. In addition, a docking study was performed to evaluate the ability of ligands to interact within the active site of cyclooxygenases (COX-1 and COX-2). Docking results showed a possible binding of stannoxanes theoretically more selective towards COX-2 than ibuprofen.
- Romero-Chávez, Maria M.,Pineda-Urbina, Kayim,Pérez, David J.,Obledo-Benicio, Fernando,Flores-Parra, Angelina,Gómez-Sandoval, Zeferino,Ramos-Organillo, ángel
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- Synthesis, characterization, and biological evaluation of furoxan coupled ibuprofen derivatives as anti-inflammatory agents
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A series of furoxan-based nitric oxide releasing ibuprofen derivatives were synthesized and tested for their anti-inflammatory, analgesic, ulcerogenic, lipid peroxidation, and hepatotoxic properties. The compounds exhibited more protection than ibuprofen with regard to gastric toxicity. Among the tested compounds 4-[2-[2-(4-isobutylphenyl)propanamido]ethoxycarbonyl]-3-methylfuroxan and 4-[2-[2-(4-isobutylphenyl)propanoyl]hydrazinecarbonyl]-3-phenylfuroxan emerged as most active anti-inflammatory agents with reduced gastrotoxicity. The results showed that incorporation of NO donating group caused a moderate increase in anti-inflammatory activity with a marked decrease in gastric ulcerations compared to their parent drug ibuprofen. A molecular docking study of all the compounds was also performed to provide the binding modes of COX-1 enzyme. Among all the titled compounds, 4-[2-[2-(4-isobutylphenyl)propanamido]ethoxycarbonyl]-3-methylfuroxan was found to be most potent and have high docking score showing favorable orientation within the COX-1 binding site.
- Amir, Mohd,Akhter, Mohd Wasim,Alam, Ozair
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p. 493 - 508
(2016/03/19)
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- SYSTEMS AND METHODS FOR AMELIORATING THE EFFECTS OF TOBACCO PRODUCTS
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The present invention provides a composition comprising a nicotine-containing material and an anti-cancer agent usable in the treatment and/or prevention or reduction of the risk of cancer and precancerous conditions as well as for preventing or reducing
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Page/Page column 86
(2015/12/08)
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- Synthesis of NO-NSAID dendritic prodrugs via Passerini reaction:new approach to the design of dendrimer-drug conjugates
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We report the synthesis of a novel class of dendritic prodrugs via Passerini reaction in one pot. Such dendrimers feature a simultaneous attachment of a conventional non-steroidal anti-inflammatory drug (NSAID) (such as ibuprofen and aspirin) and a nitric oxide (NO)-releasing moiety (such as an organic nitrate) onto their surface, and are therefore regarded as new drug delivery systems for NO-releasing NSAIDs (NO-NSAIDs).
- Du, Zuyin,Yanhui, Lu,Dai, Xuedong,Zhang-Negrerie, Daisy,Gao, Qingzhi
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p. 181 - 185
(2013/07/05)
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- Application of Oxidative Aryl Migration in Organo-selenium and -tellurium Compounds to the Synthesis of 2-Arylpropanoic Acids
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The ethylene acetals of aryl α-phenylseleno- and α-phenyltelluro-ethyl ketones i, Ph, Br) and 5-bromo-6-methoxy-2-naphthyl> have been prepared in 12-83percent yields by treating the corresponding α-bromo compounds with diphenyl diselenide-sodium or diphenyl ditelluride-sodium, respectively, in tetrahydrofuran-dimethylformamide under reflux for 6-10 h, during which the bromine is substituted by the PhSe or PhTe group.This substitution is not observed when the (PhM)2-NaBH4-EtOH (M=Se, Te) system which is known as a source of PhM- anion is used.Oxidation of the acetals thus formed with an excess of meta-chloroperbenzoic acid at 20-25 deg C for 1 h affords hydroxy-ethyl 2-arylpropanoates in 56-86percent yields via aryl group migration which are hydrolysed to 2-arylpropanoic acids, some of which are pharmaceutically important compounds.Overall isolated yields of 2-arylpropanoic acids are around 30-42percent based on the starting propiophenones over 5 steps.
- Uemura, Sakae,Fukuzawa, Shin-ichi,Yamauchi, Takayoshi,Hattori, Kaneaki,Mizutaki, Shoichi,Tamaki, Kentaro
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p. 1983 - 1987
(2007/10/02)
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- New Preparative Method for 2-Arylpropanoic Acids by Oxidative Aryl Migration in Aryl α-Seleno- and Aryl α-Telluro-ethyl Ketones
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Oxidation with m-chloroperbenzoic acid of the ethylene acetals of aryl α-phenylseleno- or aryl α-phenyltelluro-ethyl ketones prepared by treating the corresponding α-bromo compounds with diphenyl diselenide-sodium or diphenyl ditelluride-sodium, respectively, affords hydroxyethyl 2-arylpropanoates in moderate to good yields via aryl group migration.
- Uemura, Sakae,Fukuzawa, Shin-ichi,Yamauchi, Takayoshi,Hattori, Kaneaki,Mizutaki, Shoichi,Tamaki, Kentaro
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p. 426 - 427
(2007/10/02)
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