76167-92-5Relevant academic research and scientific papers
Chiral inversion of 2-arylpropionyl-CoA esters by human α-methylacyl-CoA racemase 1A (P504S) - A potential mechanism for the anti-cancer effects of ibuprofen
Woodman, Timothy J.,Wood, Pauline J.,Thompson, Andrew S.,Hutchings, Thomas J.,Steel, Georgina R.,Jiao, Ping,Threadgill, Michael D.,Lloyd, Matthew D.
, p. 7332 - 7334 (2011)
Metabolic chiral inversion of 2-arylpropanoic acids (2-APAs; 'profens'), such as ibuprofen, is important for pharmacological activity. Several 2-APA-CoA esters were good racemisation substrates for human AMACR 1A, suggesting a common chiral inversion pathway for all 2-APAs and an additional mechanism for their anti-cancer properties.
Antipyretic and analgesic ibuprofen-beta-cyclodextrin secondary-side derivative and preparation method thereof
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Paragraph 0040-0043; 0046-0047; 0049-0050; 0052-0053, (2019/10/10)
The invention provides an antipyretic and analgesic ibuprofen-beta-cyclodextrin secondary-side derivative and a preparation method thereof. An intermediate product ibuprofen imidazolate is prepared from ibuprofen and CDI (1,1'-carbonyldiimidazole) as raw
A novel long-acting analgesic ibuprofen composition and its preparation method (by machine translation)
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Page/Page column 6; 8; 9, (2019/10/17)
A novel long-acting analgesic composition of ibuprofen, 2nd surface by the ibuprofen - β - cyclodextrin derivatives, ibuprofen composition, the invention also discloses a novel long-acting analgesic ibuprofen composition preparation method, first to ibupr
Ultrasound-assisted, convenient and widely applicable 1,1′-carbonyl-diimidazole-mediated "One-pot" syntheses of acyl/sulfonyl hydrazines
Khan, Khalid Mohammed,Salar, Uzma,Fakhri, Muhammad Imran,Taha, Muhammad,Hameed, Abdul,Perveen, Shahnaz,Voelter, Wolfgang
, p. 637 - 644 (2015/11/09)
Acyl / sulfonyl hydrazines were synthesized in a one-pot reaction from carboxylic acid/aryl sulfonic acid in the presence of 1,1′-carbonyl diimidazole (CDI) under ultrasound as well as under conventional heating. The reaction was performed on diverse organic molecules including simple benzoic acid (1), electron-donating and electron-withdrawing substituted benzoic acids, biologically active compounds like coumarin-3-carboxylic acid (12), 7-hydroxycoumarin-4-acetic acid (13), and therapeutic drugs like ibuprofen (14), flurbiprofen (15), naproxen (16) or tricyclic adamantane carboxylic acid (17). Benzene sulfonic acid (18) and its derivatives (19, 20, 21 and 22) were used to prepare corresponding sulfonyl hydrazide. All products were synthesized in very good yield via ultrasonic irradiation method and characterized by spectroscopic techniques including EIMS, 1H NMR, 13C NMR, IR. The method was found very simple, facile, efficient and high yielding (>90).
Chondroitin sulfate-based anti-inflammatory macromolecular prodrugs
Peng, Yu-Shiang,Lin, Shih-Chun,Huang, Shih-Jer,Wang, Yu-Ming,Lin, Ying-Jer,Wang, Li-Fang,Chen, Jenn-Shing
, p. 60 - 69 (2007/10/03)
Macromolecular prodrugs of three non-steroidal anti-inflammatory drugs (NSAIDs), ibuprofen, ketoprofen, and naproxen, were prepared by the covalent attachment of the drugs onto chondroitin sulfate (ChS) using PEG 1000 as a spacer. Drug-PEG adducts were synthesized using 1,1′-carbonyl diimidazole as a coupling agent in dimethyl sulfoxide, followed by the reaction with ChS in highly dilute aqueous solution at pH 6.8 via N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (EDAC) as a conjugation agent. The drug-ChS conjugates were confirmed by FTIR, 1H NMR and 13C NMR and the molar percent of drug substitution onto ChS was characterized by 1H NMR using the peak areas of the three protons of -ΦCHCH3 on the drugs to those of -NHCOCH3 on ChS. All drug-ChS conjugates are water-soluble. The release amounts of the free drugs from their corresponding drug-ChS conjugates were evaluated in the presence or absence of either esterase or chondroitinase, and the both enzymes in pH 7.4 Tris-buffer solutions at 37 °C by high performance liquid chromatography (HPLC). Keto-ChS conjugates released ～100% ketoprofen within 12 h in the presence of esterase, but the combination with chondroitinase did not accelerate the release rate. The degradation of Keto-ChS conjugates by chondroitinase was confirmed by gel permeation chromatography (GPC). The Keto-ChS conjugates still retained the enzymatic recognition even at the substitution of ketoprofen as high as 56 mol%. The inhibition percent of carrageenan-induced edema of Keto-ChS-56 was comparable to that of a simple blend of ChS and ketoprofen, suggesting that biologically active ChS and ketoprofen could be liberated from the conjugate.
