Category: 328-90-5

Cho, Hea-Young published the artcileSimultaneous determination of triflusal and its major active metabolite, 2-hydroxy-4-trifluoromethyl benzoic acid, in rat and human plasma by high-performance liquid chromatography, HPLC of Formula: 328-90-5, the publication is Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences (2003), 798(2), 257-264, database is CAplus and MEDLINE.

A rapid, selective and sensitive HPLC method was developed and validated for the simultaneous determination of triflusal and its major active metabolite, 2-hydroxy-4-trifluoromethyl HOBz (HTB), in rat and human plasma. HPLC anal. was carried out using a 5-μm particle size, C₁₈-bonded SiO₂ column and MeCN-MeOH-H₂O (25:10:65, volume/volume/v) as the mobile phase and UV detection at 234 nm. Furosemide was used as the internal standard The method involved extraction with an MeCN-CHCl₃ mixture (60:40, volume/volume) and evaporation to dryness with N stream. The chromatograms showed good resolution and sensitivity and no interferences by plasma constituents. The mean absolute recovery for human plasma was 93.5 ± 4.2% for triflusal and 98.5 ± 3.1% for HTB. The lower limits of quantification of triflusal and HTB in human plasma were 20 and 100 ng/mL, resp. The calibration curves in human plasma were linear over the concentration range 0.02-5.0 μg/mL for triflusal and 0.1-200.0 μg/mL for HTB with correlation coefficients >0.999 and with inter- or intra-day coefficients of variation (CV) not exceeding 10.0%. This assay procedure was applied to the study of metabolite pharmacokinetics of triflusal and HTB in rat and human.

Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences 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

Cho, Hea-Young published the artcileGastrointestinal and hepatic first-pass effects of triflusal in rats, SDS of cas: 328-90-5, the publication is Yakche Hakhoechi (2001), 31(4), 265-271, database is CAplus.

In order to elucidate the influence of intestinal and hepatic first-pass effect on the pharmacokinetics of triflusal, the biotransformation of triflusal in the gastrointestinal tract and liver was designed. Moreover, we tried to establish an HPLC method applicable for bioassay and available to pharmacokinetics, not only with the simultaneous determination of triflusal and its active metabolite, 2-hydroxy-4-trifluoromethyl benzoic acid (HTB), but also with improving sensitivity. After the administration of triflusal (10 mg/kg) and HTB (10 mg/kg) into femoral vein, portal vein (only triflusal) and oral route (only triflusal), pharmacokinetic parameters were investigated from the plasma concentration-time profiles of triflusal and HTB in rats. An HPLC method was developed for the simultaneous determination of triflusal and HTB in rat plasma, urine and bile. The HPLC anal. was carried out using a C18 column and acetonitrile-methanol-water (25:10:65, volume/volume/v) as the mobile phase and UV detection at 234 nm. Furosemide was used as the internal standard The calibration curves were linear over the concentration range 0.05-5.0 μg/mL for triflusal and 0.2-200.0 μg/mL for HTB with correlation coefficients greater than 0.999 and with intra-day or inter-day coefficients of variation not exceeding 10.0%. This assay procedure was applied to the study of metabolite pharmacokinetics of triflusal and HTB in rats. It was supposed that triflusal was almost metabolized in vivo because urinary and biliary excreted amounts of triflusal could be ignored as it was lower than 1.2 % of the administered dose. According to the gastrointestinal and hepatic biotransformation pathways of triflusal, it was found that triflusal was hydrolyzed by about 5 % in intestine and metabolized by about 53 % in liver, and that the bioavailability of triflusal after oral administration of triflusal was 0.44, and also that the fraction of total elimination rate of triflusal which formed HTB in liver (F_mi, %) was about 98%. These results showed that triflusal was almost metabolized in liver, and the total elimination of triflusal in the body was dependent to the formation rate of HTB from triflusal in liver.

Yakche Hakhoechi 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

Oh, Soo-Jin published the artcileMONNA, a potent and selective blocker for transmembrane protein with unknown function 16/anoctamin-1, HPLC of Formula: 328-90-5, the publication is Molecular Pharmacology (2013), 84(5), 726-735, database is CAplus and MEDLINE.

Transmembrane protein with unknown function 16/anoctamin-1 (ANO1) is a protein widely expressed in mammalian tissues, and it has the properties of the classic calcium-activated chloride channel (CaCC). This protein has been implicated in numerous major physiol. functions. However, the lack of effective and selective blockers has hindered a detailed study of the physiol. functions of this channel. In this study, we have developed a potent and selective blocker for endogenous ANO1 in Xenopus laevis oocytes (xANO1) using a drug screening method we previously established. We have synthesized a number of anthranilic acid derivatives and have determined the correlation between biol. activity and the nature and position of substituents in these derived compounds A structure-activity relationship revealed novel chem. classes of xANO1 blockers. The derivatives contain a -NO₂ group on position 5 of a naphthyl group-substituted anthranilic acid, and they fully blocked xANO1 chloride currents with an IC₅₀ < 10 μM. The most potent blocker, N-((4-methoxy)-2-naphthyl)-5-nitroanthranilic acid (MONNA), had an IC₅₀ of 0.08 μM for xANO1. Selectivity tests revealed that other chloride channels such as bestrophin-1, chloride channel protein 2, and cystic fibrosis transmembrane conductance regulator were not appreciably blocked by 10∼30 μM MONNA. The potent and selective blockers for ANO1 identified here should permit pharmacol. dissection of ANO1/CaCC function and serve as potential candidates for drug therapy of related diseases such as hypertension, cystic fibrosis, bronchitis, asthma, and hyperalgesia.

Molecular Pharmacology 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

Luo, Feihua published the artcilePalladium-catalyzed ortho-C-H hydroxylation of benzoic acids, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is Tetrahedron Letters (2021), 153434, database is CAplus.

A simple Pd(OAc)₂ catalyzed ortho-hydroxylation of benzoic acids using TBHP as the sole oxidant was explored. This protocol featured relatively broad substrate scope and operational simplicity. The compatibility of ortho-substituted substrates was an effective complement to the previous ortho-hydroxylation reaction.

Tetrahedron Letters 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

Guo, Xiao-xia published the artcileNew highly phosphorescent heteroleptic tris-cyclometalated iridium(III) complexes: Synthesis and photophysical characterization, Product Details of C8H5F3O3, the publication is Guangpuxue Yu Guangpu Fenxi (2010), 30(1), 170-173, database is CAplus and MEDLINE.

New heteroleptic tris-cyclometalated iridium(III) complexes (ppy)₂Ir(LX) [ppy = 2-phenylpyridine, LX = Sal (salicylic acid), MSal (4-methylsalicylic acid), FSal (4-trifluoromethylsalicylic acid)] was synthesized and characterized. The mol. structure, photophys. properties and thermal stability were tested and analyzed. The results show that the absorption peaks were located around 270, 370, 450 and 484 nm resp. at room temperature The two former peaks at 270 and 370 nm should belong to ¹π^–π^* transition at ppy and transition from salicylic acid ligands to 2-phenylpyridine. The peaks around 450 and 484 nm can be assigned to the charge transfer transition from Ir to ligand (¹MLCT and ³MLCT) and ³π^–π^* transition resp. The PL emission peaks were located at 520, 522, and 510 nm, resp. The emission of (ppy)₂Ir(Sal) and (ppy)₂Ir(MSal) was mainly ascribed to the radiation transition of triple state ³MLCT, while the emission of (ppy)₂ Ir(FSal) was mainly from the radiation transition between Sal and ppy, partly from the radiation transition of single state ¹MLCT and triple state ³MLCT. The quantum efficiencies of these complexes were 0.37, 0.33 and 0.29 resp. The thermal decomposition temperature was from 306 to 328°C. (ppy)₂Ir(LX), being efficient phosphorescent materials with good thermal stability, can be used in organic electroluminescent devices.

Guangpuxue Yu Guangpu Fenxi 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, Product Details of C8H5F3O3.

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

Yu, Jian-ning published the artcileA new type of iridium (III) phenylpyrazole complexes: synthesis, photophysical characterization, Category: alcohols-buliding-blocks, the publication is Guangpuxue Yu Guangpu Fenxi (2010), 30(9), 2424-2427, database is CAplus and MEDLINE.

New heteroleptic iridium(III) complexes (ppz)₂Ir(LX), which consist of two cyclometalated ligands ppz(1-pheny-lpyrazole) together with an ancillary ligand LX (LX=2-(2′-hydroxylphenyl)benzothiazole (BTZ),2-(3′-methyl-2′-hydroxyl-phenyl) benzothiazole (3-MeBTZ), 2-(4′-methyl-2′-hydroxylphenyl)benzothiazole (4-MeBTZ) and 2-(4′-Trifluoromcthyl-2′-hydroxylphenyl)benzothiazole (4-tfmBTZ)), were synthesized and characterized. The mol. structures and photophys. properties were characterized and analyzed comparatively. The results show that the four complexes have basically similar UV-Vis absorption spectra, fluorescence excitation and emission spectra. Their maximum emission peaks are located at 583-615 nm, and accompanied by a lower intensity emission band around 400 nm. The weak emissions around 400 nm are ascribed to the radiation transition of single state excition from ancillary ligand BTZ perturbed by metallic ion, and light emission around long-wavelength to the radiation transition of ³MLCT of Ir(BTZ) fragment. While the triplet state ³MLCT of Ir(ppz)₂ fragment might be quenched at room temperature For all complexes, the excitations with maximum efficiency are located at 250-310 nm, which indicates that main contributor to light emitting is ligand-centered absorption(¹π-π^*) of ppz and BTZ rather than ³MLCT transitions, and thus provides a striking evidence that there is intersystem crossing from ¹π-π^* state to ³MLCT state in these complexes. Compared with Ir(ppz)₃, these complexes not only have stronger phosphorescence at room temperature but also their emission color can be tuned by modifying ancillary ligand.

Guangpuxue Yu Guangpu Fenxi 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 C10H2F12NiO4, Category: alcohols-buliding-blocks.

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

Gormemis, Ahmet E. published the artcileBenzofuroindole analogues as potent BK_Ca channel openers, Recommanded Product: 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is ChemBioChem (2005), 6(10), 1745-1748, database is CAplus and MEDLINE.

New, potent, large-conductance, calcium-activated potassium-channel (BK_Ca) openers that show calcium-independent activation in electrophysiol. evaluations have been designed through optimizing the structure of the benzofuroindole skeleton by comparison with a known BK_Ca-channel opener (BMS-204352). A series of substituted benzofuroindoles I (R¹ = H, Br; R² = H, CF₃, OCH₃, Cl; R³ = H, COOH, COOCH₃, Cl, OCH₃, CF₃; R⁴ = H, Cl, F; R⁵ = H, Cl, CF₃; R⁶ = H, Cl, F, CF₃) were prepared via sequence of reactions including as a key step either classical Fischer indole or microwave assisted cyclization of phenylhydrazones of benzofuranones. The BK_Ca-channel-opening activities of synthesized benzofuroindoles were studied. In particular, compound I (R¹ = R⁴ = R⁵ = H; R² = CF₃; R³ = COOH, R⁶ = Cl) showed the most potent and effective activity in an intracellular calcium-independent manner. These new potassium channel openers might find therapeutic use to treat neuronal damage and be applied to therapeutic intervention in stroke, asthma, hypertension, convulsion, and traumatic brain injury.

ChemBioChem 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, Recommanded Product: 2-Hydroxy-4-(trifluoromethyl)benzoic acid.

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

Qiao, Chunhua published the artcile5′-O-[(N-Acyl)sulfamoyl]adenosines as Antitubercular Agents that Inhibit MbtA: An Adenylation Enzyme Required for Siderophore Biosynthesis of the Mycobactins, SDS of cas: 328-90-5, the publication is Journal of Medicinal Chemistry (2007), 50(24), 6080-6094, database is CAplus and MEDLINE.

A study of the structure-activity relationships of 5′-O-[N-(salicyl)sulfamoyl]adenosine (6), a potent inhibitor of the bifunctional enzyme salicyl-AMP ligase (MbtA, encoded by the gene Rv2384) in Mycobacterium tuberculosis, is described, targeting the salicyl moiety. A systematic series of analogs was prepared exploring the importance of substitution at the C-2 position revealing that a hydroxy group is required for optimal activity. Examination of a series of substituted salicyl derivatives indicated that substitution at C-4 was tolerated. Consequently, a series of analogs at this position provided 4-fluoro derivative, which displayed an impressive MIC₉₉ of 0.098 μM against whole-cell M. tuberculosis under iron-limiting conditions. Examination of other heterocyclic, cycloalkyl, alkyl, and aminoacyl replacements of the salicyl moiety demonstrated that these nonconservative modifications were poorly tolerated, a result consistent with the fairly strict substrate specificities of related nonribosomal peptide synthetase adenylation enzymes.

Journal of Medicinal 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 C8H5F3O3, SDS of cas: 328-90-5.

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

Lynch, John K. published the artcileOptimization of Chromone-2-carboxamide Melanin Concentrating Hormone Receptor 1 Antagonists: Assessment of Potency, Efficacy, and Cardiovascular Safety, Computed Properties of 328-90-5, the publication is Journal of Medicinal Chemistry (2006), 49(22), 6569-6584, database is CAplus and MEDLINE.

Evaluation of multiple structurally distinct series of melanin concentrating hormone receptor 1 antagonists in an anesthetized rat cardiovascular assay led to the identification of a chromone-2-carboxamide series as having excellent safety against the chosen cardiovascular endpoints at high drug concentrations in the plasma and brain. Optimization of this series led to considerable improvements in affinity, functional potency, and pharmacokinetic profile. This led to the identification of a 7-fluorochromone-2-carboxamide (I) that was orally efficacious in a diet-induced obese mouse model, retained a favorable cardiovascular profile in rat, and demonstrated dramatic improvement in effects on mean arterial pressure in our dog cardiovascular model compared to other series reported by our group. However, this analog also led to prolongation of the QT interval in the dog that was linked to affinity for hERG channel and unexpectedly potent functional blockade of this ion channel.

Journal of Medicinal 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 C8H5F3O3, Computed Properties of 328-90-5.

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

Enache, Teodor Adrian published the artcileElectrochemical behavior of triflusal, aspirin and their metabolites at glassy carbon and boron doped diamond electrodes, Synthetic Route of 328-90-5, the publication is Combinatorial Chemistry & High Throughput Screening (2010), 13(7), 569-577, database is CAplus and MEDLINE.

The electrochem. behavior of triflusal (TRF) and aspirin (ASA), before and after hydrolysis in water and in alk. medium using two different electrode surfaces, glassy carbon and boron doped diamond, was studied by differential pulse voltammetry over a wide pH range. The hydrolysis products were 2-(hydroxyl)-4-(trifluoromethyl)-benzoic acid (HTB) for triflusal and salicylic acid (SA) for aspirin, which in vivo represent their main metabolites. The hydrolysis processes were also followed by spectrophotometry. The UV results showed complete hydrolysis after one hour for TRF and after two hours for ASA in alk. solution The glassy carbon electrode enables only indirect determination of TRF and ASA through the electrochem. detection of their hydrolysis products HTB and SA, resp. The oxidation processes of HTB and SA are pH dependent and involve different numbers of electrons and protons. Moreover, the difference between the oxidation peak potential of SA and HTB was equal to 100 mV in the studied pH range from 1 to 8 due to the CF₃ of the aromatic ring of HTB mol. Due to its wider oxidation potential range, the boron doped diamond electrode was used to study the direct oxidation of TRF and ASA, as well as of their resp. metabolites HTB and SA.

Combinatorial Chemistry & High Throughput Screening 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, Synthetic Route of 328-90-5.

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