Category: 328-90-5

Argemi, Anna published the artcileSpectroscopic and chromatographic characterization of triflusal delivery systems prepared by using supercritical impregnation technologies, Application In Synthesis of 328-90-5, the publication is Journal of Pharmaceutical and Biomedical Analysis (2008), 46(3), 456-462, database is CAplus and MEDLINE.

This study describes the development and evaluation of an anal. method for the characterization of triflusal (2-acetoxy-4-(trifluoromethyl) benzoic acid) dispersed in sustained delivery systems prepared using supercritical fluid impregnation technol. Characterization assays comprised the determination of the percentage of triflusal and its degradation product impregnated in polymeric supports and further monitoring of the releases of the 2 drug components over time in physiol. conditions. Preliminary delivery profiles were monitored spectrophotometrically using a continuous-flow system. In this case, no selective wavelength for discriminating between triflusal and metabolite was found so that measurements at 225 nm provided overall profiles corresponding to the 2 compounds For a more accurate study, a chromatog. method was developed for monitoring the evolution of the concentration of the 2 components independently. Triflusal and metabolite were separated in a C₁₈ column and 25 mM acetic acid/acetate (pH 5.0) + methanol (40/60 volume/volume) mobile phase. Several triflusal-polymer samples were prepared under different exptl. conditions and release features were evaluated. Excellent delivery systems were obtained with poly(methyl)methacrylate beads treated at 40°C and 190 bar for 48 h using supercritical carbon dioxide as a solvent. These samples showed a constant sustained release of drug for several weeks.

Journal of Pharmaceutical and Biomedical Analysis published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, Application In Synthesis of 328-90-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Fernandez-Real, Jose-Manuel published the artcileSalicylates increase insulin secretion in healthy obese subjects, HPLC of Formula: 328-90-5, the publication is Journal of Clinical Endocrinology and Metabolism (2008), 93(7), 2523-2530, database is CAplus and MEDLINE.

Context: Conflicting results on the effects of salicylates on glucose tolerance in subjects with normal glucose tolerance or type 2 diabetes have been reported. Objective: The objective of the study was to investigate the effects of a salicylate derivative (triflusal) on insulin sensitivity and insulin secretion. Design, Setting, and Participants: This was a double-blind, randomized, crossover study with three treatment periods corresponding to two dose levels of triflusal and placebo in healthy obese subjects. Main Outcome Measures: Insulin sensitivity and insulin secretion, evaluated through frequently sampled iv glucose tolerance test that was performed after each treatment period, were measured. Insulin secretion was also evaluated in vitro in mice and human islets of Langerhans. Results: The administration of triflusal led to decreased fasting serum glucose concentration in the study subjects. Insulin sensitivity did not significantly change after each treatment period. Insulin secretion, however, significantly increased in a dose-dependent fashion after each triflusal treatment period. The administration of 800 μM of the main triflusal metabolite to whole mice islets of Langerhans led to a sustained increase in intracellular calcium concentration level. This was followed by a significantly increase in insulin secretion. In human islets, 200 μM of 2-hydroxy-4-trifluoromethylbenzoic acid was sufficient to increase insulin release. Conclusions: The administration of a salicylate compound led to lowering of serum glucose concentration We suggest that this effect was mediated through increased insulin secretion induced by salicylate directly on the β-cell.

Journal of Clinical Endocrinology and Metabolism published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, HPLC of Formula: 328-90-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Murillo-Cremaes, Nerea published the artcileNanostructured silica-based drug delivery vehicles for hydrophobic and moisture sensitive drugs, SDS of cas: 328-90-5, the publication is Journal of Supercritical Fluids (2013), 34-42, database is CAplus.

Facile and robust fabrication methodologies of complex materials with high added value for controlled drug delivery systems are highly sought-after in the pharmaceutical industry. Here, the authors have relied on the use of supercritical fluids for the matrix synthesis as well as for the drug impregnation process. As a model system of a hydrophobic and moisture sensitive active agent, triflusal was impregnated in different aerogel and polymeric matrixes using supercritical CO₂. In vitro release profiles of drug carriers consisting of SiO₂ aerogels as mesoporous monoliths and as microporous nanospheres loaded with triflusal are reported and compared to a more conventional polymeric system (PMMA). Silica-based matrixes are found to prevent the hydrolization of the active ingredient more efficiently than the polymeric matrix and displayed much faster release kinetics. Moreover, the triflusal is dispersed in a mol. form inside the silica-based materials. Such features are considered of great interest to enhance the bioavailability of low solubility drugs.

Journal of Supercritical Fluids published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, SDS of cas: 328-90-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Veres, Peter published the artcileHybrid aerogel preparations as drug delivery matrices for low water-solubility drugs, COA of Formula: C8H5F3O3, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2015), 496(2), 360-370, database is CAplus and MEDLINE.

A comprehensive study of 14 hybrid aerogels of different composition with applications in drug delivery has been carried out. The overall objective was to modulate the release behavior of drug-impregnated aerogels, from an almost instantaneous release to a semi-retarded delivery prolonged during several hours, through internal surface functionalization. The designed hybrid aerogels were composed of silica and gelatin and functionalized with either Ph, long (16) hydrocarbon chain or Me moiety. As model systems, three class II active agents (pK_a < 5.5), ibuprofen, ketoprofen and triflusal, were chosen to impregnate the aerogels. The work relied on the use of supercritical fluid technol. for both the synthesis and functionalization of the hybrid aerogels, as well as for the impregnation with an active agent using supercritical CO₂ as a solvent. For the impregnated aerogels, in vitro release profiles were recorded under gastric and intestinal pH-conditions using HPLC techniques. The release behavior observed for the three studied drugs was explained considering the measured dissolution profiles of the crystalline drugs, the aerogel composition and its functionalization. Such features are considered of great interest to tailor the bioavailability of drugs with low water solubility

International Journal of Pharmaceutics (Amsterdam, Netherlands) published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C16H24BF4Ir, COA of Formula: C8H5F3O3.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Wu, Yi-Xin published the artcileCd-Doped Polyoxotitanium Nanoclusters with a Modifiable Organic Shell for Photoelectrochemical Water Splitting, Synthetic Route of 328-90-5, the publication is Inorganic Chemistry (2021), 60(24), 19263-19269, database is CAplus and MEDLINE.

Incorporating heterometal and chromogenic groups into the titanium oxo cluster (TOC) nanomaterials is one of the effective strategies for the development of new high-performance photoelec. active materials. In this Article, the authors report the structures and photoelectrochem. (PEC) performances of a family of TOCs, including pure [Ti₁₂O₈(OEt)₁₆L₈] ({Me-Ti₁₂}) and six Cd-doped clusters formulated as [H₄Cd₂Ti₁₀O₈(OEt)₁₆(L)₈(H₂O)₂] ({Cd₂Ti₁₀}; L = salicylic acid and their derivatives). The six Cd-doped clusters are isostructural, containing the same {Cd₂Ti₁₀O₈} core, but are protected by salicylic ligands modified with different functional groups. The compositions, structures, and solution stability of these clusters were studied in detail by single-crystal x-ray diffraction and electrospray ionization mass spectrometry measurements. The embedding of heterometallic Cd(II) and chem. modification of organic protective shells can effectively regulate the PEC water oxidation activity of those clusters, with {F-Cd₂Ti₁₀} having the highest turnover number of 518.55 and the highest turnover frequency of 172.85 h^-1. The authors’ work highlights the potential of using TOCs that do not contain noble metals as water oxidation catalysts, and their catalytic activity can be regulated by structural modification.

Inorganic Chemistry published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C3H6O2, Synthetic Route of 328-90-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Wu, Huaimo published the artcileAn efficient approach for the synthesis of 1,2-dihydroxanthones enabled by one-pot Claisen condensation/cyclization reactions, Name: 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is Organic & Biomolecular Chemistry (2021), 19(18), 4126-4131, database is CAplus and MEDLINE.

In this report, a mild, efficient and green method for the synthesis of 1,2-dihydroxanthones (DHXs) I (R = H, Me, 3-methylbut-2-en-1-yl; R¹ = H, Me; R² = Me, Ph, 2,2,2-trifluoroethyl, but-3-en-1-yl, etc.; R³ = H, Me; R⁴ = H, F, OMe, Cl, Br, I; R⁵ = H, Me, OMe, Cl, CF₃, F; R⁴R⁵ = -CH:CHCH:CH-; R⁶ = H, Cl, Me, prop-2-en-1-yl) and II (R⁷ = H, OMe) has been developed in one pot through Claisen condensation and O-cyclization under waste-induced relay catalysis with min. organic solvents. The byproduct (HMDS or NH₃·H₂O) of the first step turned out to be the promoter for the second step, which could efficiently proceed in aqueous media without the addition of other catalysts. The reactions using trifluoroethyl salicylates 2-OH-3-R⁶-4-R⁵-5-R⁴-6-R³C₆HC(O)OCH₂CF₃ could be performed under mild conditions to ensure the generation of vulnerable DHXs I and II in high yields. The substrate scope is very broad regardless of the substituent type and its position on the structure. Specifically, the versatility of DHXs I (R = R¹ = R³ = R⁴ = R⁵ = R⁶ = H; R² = Me) was demonstrated by their conversion to xanthones I (R = 3-methylbut-2-en-1-yl; R¹ = R³ = R⁴ = R⁵ = R⁶ = H; R² = Me)/II (R⁷ = H) and other complex structures III/IV.

Organic & Biomolecular Chemistry published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C18H28BNO2, Name: 2-Hydroxy-4-(trifluoromethyl)benzoic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Huang, Xi-Shou published the artcileThe synthesis, structure and activity evaluation of secnidazole derivatives as Helicobacter pylori urease inhibitors, Application In Synthesis of 328-90-5, the publication is Current Bioactive Compounds (2011), 7(4), 268-280, database is CAplus.

Various secnidazole derivatives were synthesized and evaluated for Helicobacter pylori (H. pylori) urease inhibitory activities and anti-inflammatory activities. The most potent urease inhibitory activities and anti-inflammatory activities were in the range of IC₅₀ = 1.0-2.0 μM and 59-72% inhibition, resp. Docking simulation was performed with one of the compounds into the urease active site to determine the probable binding model. The compounds with potent inhibitory activity against H. pylori may be potential antibacterial agents.

Current Bioactive Compounds published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, Application In Synthesis of 328-90-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Cheng, Jinling published the artcileA Single 2-(2′-Hydroxyphenyl)benzothiazole Derivative Can Achieve Pure White-Light Emission, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is Chemistry – An Asian Journal (2014), 9(11), 3215-3220, database is CAplus and MEDLINE.

The synthesis and photophysics of two novel 2-(2′-hydroxyphenyl)benzothiazole (HBT) derivatives are presented. The electron-withdrawing trifluoromethyl (CF₃) group in compound 1 facilitates the deprotonation of the phenolic hydroxy group. Well-resolved triple fluorescence from the enol, keto, and phenolic anion, which ranges from 350 to 600 nm, was detected for 1 in ethanol, which marks the first time triple fluorescence from an excited-state intramol. proton transfer (ESIPT) mol. was reported. Both triphenylamine and CF₃ were introduced into derivative 2. Intramol. charge transfer and the “red-edge effect” resulted in the bathochromic shift of dual fluorescence of 2. Triple fluorescence was also observed for 2 in ethanol. In mixed acetonitrile and ethanol, pure white-light emission with CIE coordinates of (0.33, 0.33) and a quantum yield of 0.25 was achieved for 2. This work provides a new avenue for the rational design of an ESIPT mol. to achieve white-light generation under mild conditions.

Chemistry – An Asian Journal published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Cheng, Jinling published the artcileComprehensive Studies on Excited-State Proton Transfer of a Series of 2-(2′-Hydroxyphenyl)benzothiazole Derivatives: Synthesis, Optical Properties, and Theoretical Calculations, Safety of 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is Journal of Physical Chemistry C (2015), 119(8), 4242-4251, database is CAplus.

A group of novel 2-(2′-hydroxyphenyl)benzothiazole derivatives (1-4) with excited-state intramol. proton transfer (ESIPT) character were synthesized. Their photophys. properties were studied by means of steady-state absorption and fluorescence spectra and time-resolved emission method as well as theor. calculation in a variety of solvents. All of these compounds can yield single fluorescence at the green region in nonpolar solvents such as n-hexane, while dual fluorescence consisting of the blue and green bands was captured in strong polar solvents like acetonitrile. In addition, a third emission band between the former two bands was detected for these mols. simultaneously with the blue and green ones generating the well-structured triple fluorescence in protic solvent like ethanol. Systematical comparison of the fluorescence of these compounds in a series of solvents demonstrated that nonpolar solvents would facilitate ESIPT process and the green emission from the keto format, while the strong polar solvents impede the ESIPT process and favor the blue normal emission from enol. Protic solvents facilitate deprotonation and make the phenolic anion coexist with keto and enol and consequently lead to triple fluorescence. On the premise of identical keto emission intensity, the normal emission intensity of these compound increases consecutively in the order of increasing electron-withdrawing ability of the substituents regardless of solvents. The results of quantum-chem. calculations are well in line with the exptl. spectra.

Journal of Physical Chemistry C published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, Safety of 2-Hydroxy-4-(trifluoromethyl)benzoic acid.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Lee, Hae Won published the artcileA Phase I study to characterize the multiple-dose pharmacokinetics, pharmacodynamics and safety of new enteric-coated triflusal formulations in healthy male volunteers, SDS of cas: 328-90-5, the publication is Expert Opinion on Drug Metabolism & Toxicology (2011), 7(12), 1471-1479, database is CAplus and MEDLINE.

Objectives: An enteric-coated formulation of triflusal (triflusal EC), an antiplatelet agent, was developed to reduce the high incidence of gastrointestinal adverse events (AEs). The aim of this study is to compare the pharmacokinetics, pharmacodynamics and safety of triflusal EC with triflusal in healthy Korean male subjects to determine bioequivalence and non-inferiority for the purposes of marketing approval. Methods: A randomized, open-label, two-period, crossover study was conducted in 38 subjects. Either triflusal EC or triflusal was administered orally as a single 900 mg loading dose (day 1) followed by eight 600 mg/day maintenance doses on days 2 – 9, with a 13-day washout period. The plasma concentrations of 2-hydroxy-4-trifluoromethyl benzoic acid (HTB), the predominant active metabolite of triflusal, were assessed after administration of the loading dose, using HPLC/MS/MS. The platelet aggregation response to arachidonic acid was determined using turbidimetric aggregometry. Results: The 90% CIs, for the geometric mean ratios of the log-transformed AUC_τ and C_max of HTB were seen to be within the predetermined range of 0.8 – 1.25. Triflusal EC was also shown to be non-inferior in its anti-aggregatory effect. No serious AEs were reported during this study. Conclusions: The pharmacokinetic and pharmacodynamic profiles of the two triflusal formulations met the requirements for bioequivalence and non-inferiority, resp. Both formulations were well tolerated.

Expert Opinion on Drug Metabolism & Toxicology published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, SDS of cas: 328-90-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts