Diphenylether (DPE) was efficiently hydrolyzed into phenol (up to 58 mol%), using Lewis acids, such as boron trifluoride (BF3) and Ni(BF4)2, in supercritical water (SCW) at 380 °C. The side-reactions were insignificant, and BF3 was found to be nearly twice as effective, than HBF4 under the same...
Polyvinylpolypyrrolidone-supported boron trifluoride has been studied for synthesis of 4-methyl coumarin by the Pechmann reaction. The reaction proceeded smoothly with hydroxyl phenols and ethyl acetoacetate in good yields in ethanol at reflux conditions. The polyvinylpolypyrrolidone-boron trifl...
A series of weakly emissive, exited state intramolecular proton transfer active tetrahydrodibenzo[a,i]phenanthridin-5-yl)phenols were efficiently synthesized using 2-tetralone and substituted salicylaldehydes. These dyes were smoothly coordinated with boron trifluoride diethyletherate resulting ...
A highly efficient method for the acylation of alcohols, phenols and trimethylsilyl ethers with acetic anhydride is described using polyvinylpolypyrrolidone-bound boron trifluoride (PVPP-BF3) under mild and heterogeneous conditions at room temperature in good to excellent yields. The polyvinylpo...
An organocopper reagent, derived from allyl(diethylamino)dimethylsilane via metalation by n-BuLi/TMEDA followed by transmetalation, reacts with aldehydes regioselectively at the γ position to form 1-substituted (E)-3-buten-1-ol derivatives. Epoxidation of the double bond followed by hydrogen pe...
While there have been large amount of research activities on the chemistry and biology of catechins (flavan-3-ols/2-arylchroman-3-ols) and their derivatives, the systematic synthetic and bioevaluation studies of congeneric 4-arylchroman-3-ols remain a less explored area. Towards that objective, ...
For patient convenience, sustained release Adefovir Poly-d,l-lactic-co-glycolic acid (PLGA) microspheres were formulated to relieve the daily use of the drug which is a problem for patients treated from chronic hepatitis-B. PLGA microspheres were prepared and characterized by entrapment efficien...
Background & AimsTenofovir disoproxil fumarate (TDF) monotherapy has displayed non-inferior efficacy to TDF plus entecavir (ETV) combination therapy in patients with hepatitis B virus (HBV) resistant to ETV and/or adefovir (ADV). Nonetheless, the virologic response rate was suboptimal in patient...
Vemurafenib is a B-Raf V600E inhibitor that exerts significant inhibitory effects in melanoma but not in colon cancer, and the mechanism of vemurafenib resistance remains unclear. In this study, bioinformatics analysis of gene profiles in cancer cells treated with vemurafenib or its analog revea...
Background and aimsAdefovir, an acyclic nucleotide reverse transcriptase inhibitor used to treat hepatitis B viral infection, is primarily eliminated renally through cooperation of glomerular filtration with active tubular transport. Nonalcoholic steatohepatitis is a variable in drug disposition...
The deficiency of nucleos(t)ide analogues (NAs) as anti-hepatitis B virus (HBV) drugs in clinical use is attributable to their insufficient enrichment in liver and non-target organ toxicity. We aimed to develop potent anti-HBV adefovir derivatives with hepatotrophic properties and reduced nephro...
In this paper, two novel polymorphs of adefovir dipivoxil-saccharin (AD-SAC) cocrystals, forms II and III, were prepared and characterized by PXRD, DSC, FT-IR and SEM. Polymorphic transformations of these two forms and the known form (form I) were also investigated. In comparison to form I, form...
An effective combination pretreatment of bamboo shoot shell (BSS) using Emulsifier OP-10 (0.5%, w/v) in the acidified media (pH 4.0) by autoclaving (120 °C, 40 min) was conducted. After BSS slurry without detoxification was enzymatically hydrolyzed for 96 h, glucose (25.2 g/L) and xylose (7.5 g...
The research investigates whether the copper activation of sphalerite can result in the adsorption of xanthate on the S-site of sphalerite surface at the atomic level. The adsorption of ethyl xanthate (EX) molecule on the un-activated and Cu-activated sphalerite (1 1 0) surface in the presence o...
Anti-microbial effect is produced when the ligand (L) S-ethyl-l-cysteine sulfoxide (Ethiin) makes coordination complex with metal ‘M’ (M = Cu, Co, Ni), while, ethiin did not show any antimicrobial effect. The synthesized complexes have 1:2 metal to ligand ratio (ML2). The spectro-chemical anal...
A sensitive and specific procedure using high-performance liquid chromatography for the quantification of sulforidazine and two diastereomeric sulforidazine-5-sulfoxide metabolites in plasma was developed. Sulforidazine was first extracted from basified plasma using a mixture of pentane and 2-pr...
A synthetic peptide corresponding to Cys-thymopoietin28–39 was synthesized and coupled by diazo linkages to aminophenyl thioether-derivatized paper disks. Disks were implanted the peritoneal cavities of mice, initially after soaking in complete Freund's adjuvant and subsequently, at 3 week...
Thymopoietin-containing cells in the thymus were identified immunohistochemically using murine antiserum generated by immunization with synthetic Cys-thymopoietin28–39 (Cys-TP28–39). This antiserum, previously shown to react with both bovine and human thymopoietin, gave reactivity restricted t...
Pristine humic acids (HAs) were thermally condensed onto silica microparticles by a one-pot, inexpensive and green preparation route obtaining a mixed-mode sorbent ([email protected]) with good sorption affinity for glucocorticoids (GCs). The carbon-based material, characterized by various techn...
Seleno-l-methionine (SeMet) can be oxidized to l-methionine selenoxide (MetSeO) by flavin-containing monooxygenase 3 (FMO3) and rat liver microsomes in the presence of NADPH. MetSeO can be reduced by GSH to yield SeMet and GSSG. In the present study, the potential reduction of MetSeO to SeMet by...
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