80965-09-9Relevant academic research and scientific papers
Ketorolac beats ketoprofen: Lower photodecarboxylation, photohemolysis and phototoxicity
McTiernan, Christopher D.,Fasciani, Chiara,Gonzalez-Bejar, Maria,Roca-Sanjuan, Daniel,Alarcon, Emilio I.,Netto-Ferreira, Jose Carlos
, p. 1619 - 1622 (2013)
Ketorolac shows reduced photohemolytic activity and low phototoxicity against human skin fibroblasts when compared to ketoprofen. The low decarboxylation quantum yield together with the efficient non-radiative deactivation of the triplet and singlet excit
Dual Mechanoenzymatic Kinetic Resolution of (±)-Ketorolac
Juaristi, Eusebio,Pérez-Venegas, Mario,Rodríguez-Trevi?o, Agustín Mario
, (2020/02/15)
Recently, biocatalysis mediated by mechanical energy has become a convenient strategy to obtain highly valuable products following the principles of green chemistry. In particular, mechanoenzymatic techniques have allowed the isolation of chiral drugs wit
Characterization of forced degradation products of ketorolac tromethamine using LC/ESI/Q/TOF/MS/MS and in silico toxicity prediction
Kalariya, Pradipbhai D.,Raju,Borkar, Roshan M.,Namdev, Deepak,Gananadhamu,Nandekar, Prajwal P.,Sangamwar, Abhay T.,Srinivas
, p. 380 - 391 (2014/05/20)
Ketorolac, a nonsteroidal anti-inflammatory drug, was subjected to forced degradation studies as per International Conference on Harmonization guidelines. A simple, rapid, precise, and accurate high-performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (LC/ESI/Q/TOF/MS/MS) method has been developed for the identification and structural characterization of stressed degradation products of ketorolac. The drug was found to degrade in hydrolytic (acidic, basic, and neutral), photolytic (acidic, basic, and neutral solution), and thermal conditions, whereas the solid form of the drug was found to be stable under photolytic conditions. The method has shown adequate separation of ketorolac tromethamine and its degradation products on a Grace Smart C-18 (250-mm-×-4.6-mm i.d., 5-μm) column using 20-mM ammonium formate (pH-=-3.2): acetonitrile as a mobile phase in gradient elution mode at a flow rate of 1.0-ml/min. A total of nine degradation products were identified and characterized by LC/ESI/MS/MS. The most probable mechanisms for the formation of degradation products have been proposed on the basis of a comparison of the fragmentation of the [M-+-H]+ ions of ketorolac and its degradation products. In silico toxicity of the drug and degradation products was investigated by using topkat and derek softwares. The method was validated in terms of specificity, linearity, accuracy, precision, and robustness as per International Conference on Harmonization guidelines. Copyright
Synthesis and evaluation of anti-inflammatory and analgesic activity of 3-[(5-substituted-1,3,4-oxadiazol-2-yl-thio)acetyl]-2H-chromen-2-ones
Ingale, Nista,Maddi, Veeresh,Palkar, Mahesh,Ronad, Pradeepkumar,Mamledesai, Shivalingrao,Vishwanathswamy,Satyanarayana, Darbhamulla
experimental part, p. 16 - 36 (2012/06/04)
A novel series of 3-[(5-substituted-1,3,4-oxadiazol- 2-yl-thio)acetyl]-2H- chromen-2-one (7a-i) were synthesized by the condensation between the appropriately substituted 5-substituted-1,3,4-oxadiazolyl-2-thione (4a-i) derived from various existing NSAIDs and 3-(2-bromoacetyl)- 2H-chromen-2-one (6) under reflux in the presence of sodium ethoxide. Structure of the synthesized compounds was established on the basis of physicochemical, elemental analysis, and spectral data. The title compounds were screened for in vivo acute anti-inflammatory and analgesic activities at a dose of 200 mg/kg bw. Among the series, four compounds 7c, 7e, 7f, and 7h were found to possess a significant anti-inflammatory and analgesic activity profile. In addition, these compounds were also found to possess a less degree of ulcerogenic potential as compared to standard NSAIDs. Springer Science+Business Media, LLC 2010.
Methods for preparing 5-aroyl-1,2-dihydro-3H-pyrrolo-[1,2-A]pyrrole-1-carboxylic acids
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, (2008/06/13)
This invention pertains to methods for preparing 5-aroyl-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1-carboxylic acids represented by formula (I): STR1 In a first embodiment, the method comprises the sequential steps of cyclizing, via a free radical ring closu
Novel Syntheses of 5-Aroyl-1,2-dihydro-3H-pyrrolopyrrole-1-carboxylic Acids
Franco, Fidencio,Greenhouse, Robert,Muchowski, Joseph M.
, p. 1682 - 1688 (2007/10/02)
A fundamentally new approach to the synthesis of the title compounds was devised in which the crucial step was the intramolecular displacement of methanesulfinate ion or bromide ion by the sodium enolates of properly disposed substituted malonate esters such as 13a-13c and 20.As integral parts of the above process, a new four-carbon alkylation of the pyrrole nitrogen atom, a novel synthesis of 2-(methylthio)pyrroles, and the use of the dimethylsulfonium moiety as meta directing group in the pyrrole system were developed.
5-Aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid derivatives and process for the production thereof
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, (2008/06/13)
Novel 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds represented by the formula STR1 and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein R is hydrogen or a lower alkyl group containing from 1 to 4 car
