In the present investigation the adsorption behavior of methylene blue (MB) dye from aqueous solution onto untreated chinar leaves powder (CLP) and chinar leaves biochar (CLB) has been studied. To ...find out optimum conditions, adsorption process was carried out by varying different parameters such as contact time, adsorbent dose, concentration, temperature, salts, and pH. The equilibrium adsorption data were subjected to different popular isotherms (Langmuir, Freundlich, and Temkin) and kinetic models (pseudo-first order, pseudo-second order and intra-particle diffusion model). The thermodynamic study was also done on the adsorption process. The maximum monolayer adsorption capacities for MB dye onto given adsorbents are 1.53 mg/g (CLP) and 1.02 mg/g (CLB). Also the values of RL and n suggest favourable adsorption process of MB dye onto CLP and CLB adsorbents. The pseudo-second order kinetic model is best obeyed by both the mentioned adsorbents for MB dye adsorption with R2 value equal to 1. Thermodynamic study reveals that the adsorption process of MB dye is spontaneous, endothermic (CLB) and exothermic (CLP). At an equilibrium time of 20 min the uptake efficiency (> 99%) was recorded for both the low cost adsorbents (CLP and CLB) thus proved them fast and effective adsorbents for the removal of MB dye.
The present review article is related with the method of preparation, importance and medicinal application of indole and indazoles. The studies of heterocycles is an evergreen field in the branch of ...organic chemistry and always attract the attention of chemists working not only in the area of natural products but also in the synthetic chemistry. Moreover many useful drugs have emerged from the successful investigation carried out in this branch. The derivatives of indoles and indazoles exhibits antibacterial, anticancer, antionidants, anti-inflammatory, antidiabetic, antiviral, atniproliferative, antituberculosis, antispermetogenic activity, antipsychotic drugs etc.
In the present article synthesis and medicinal applications of 1, 2, 4 oxadiazoles are reviewed. The oxadiazoles have a wide range of applications such as Antitussive, Anti-inflammatory, Anaesthetic, ...Vasodilator, anthelmintic, antiallergic, antiplatelet effects in vitro, antithrombotic properties in vivo, etc. Many researchers have synthesized novel heterocyclic compounds containing oxadiazoles with the concept of bioisosterism.
Background
A novel gradient, high-sensitive and specific stability-indicating reverse-phase HPLC method was developed and validated for quantitative purpose of known, unknown and degradant impurities ...profiling for diltiazem hydrochloride tablets. The impurities were separated on the Zorbax RX C8 column (150 mm × 4.6 mm, 5 μm) with mobile phase-A consisting of a mixture of 0.05 M sodium dihydrogen phosphate monohydrate buffer pH 3.0 and methanol in the ratio 800:200v/v and mobile phase-B consisting of acetonitrile with a flow rate of 1.0 mL min
−1
. The column compartment was maintained at 35 °C, and the detection wavelength was 240 nm. Diltiazem hydrochloride, its known impurities and unknown impurities have been well resolved from each other.
Results
The linearity of the method has been demonstrated across the concentration range of 0.18 to 5.65 µg mL
−1
for EP impurity-F with correlation coefficient
R
2
greater than 0.99. Recovery of method was proved from LOQ to 150% for known and unknown impurities with respect to test concentration and found in between 80 and 120%. Forced degradation study and specificity experiment results with mass balance proved the stability-indicating nature of the method and separated all known, unknown impurities and degradants from each other as well as from main drug component (diltiazem hydrochloride). The mass balance for stress study was found in between 95 and 105%.
Conclusion
Newly developed analytical method was validated as per ICH Q2 (R1) guidelines “Validation of analytical procedure” and found linear, accurate, specific, robust and precise in the established working range.
Novel Schiff bases of metformin hydrochloride and (
)
-nitrobenzaldehyde were synthesized by employing two efficient environmentally friendly methods, namely, stirring and microwave-assisted methods ...using water as the solvent. The advantage of microwave irradiation over the other methods was represented in the reduction of reaction time and wastes, and good yields; however, water in both methods plays the role of eco-friendly solvent. The structural properties of the (
)
-isomer products were analyzed by elemental analysis, Fourier transform infrared (FTIR) spectroscopy, UV-Visible (UV-Vis) spectroscopy,
H nuclear magnetic resonance (NMR) spectroscopy,
C NMR spectroscopy, mass spectroscopy, and differential scanning calorimetry (DSC). The newly synthesized compounds were screened for their antibacterial activity against selected Gram-positive (ATCC 25923, ATCC 43300, and ATCC 29212) and Gram-negative (ATCC 25922, ATCC 27853, and ATCC 700603) bacteria using the agar well diffusion method. Compared with the standard drug streptomycin, both Schiff bases exhibited moderate bactericidal activity against the tested bacteria with higher values of
-nitro compared with the
-nitro isomer; however, no effect on ATCC 43300 and ATCC 27853 was observed under the experimental conditions employed.
Objective: To investigate the effect of temperature and pressure on supercritical CO2 extraction of Triognella foenum graecum Linn seeds, to determine the optimal condition which leads to highest ...percentage of the accumulative yield and revealing the chemical composition of supercritical CO2 extract.Methods: Temperatures in the range of 40–60C and pressures in the range of 10–25 MPa were used. FTIR and GC–MS analysis were used to detect the bioactive compounds present in the extract. The broth dilution method and slope method were used to evaluate the anti-microbial and anti-tuberculosis activities and the in vitro anti-malarial assay was carried out according to the micro assay protocol of Rieckmann and his coworkers.Results: The temperature was more affected than the pressure on the extraction performance and the highest yield of the extract（3.111%） was attained at 60C and 10 MPa.FTIR and GC–MS showed that the chemical composition of the extract included conjugated linoleic acid methyl ester as the major active principle（with concentration of72.28%）, followed by saturated fatty acid methyl esters（16.03%）, steroids（8.09%） and organic siloxane compound（3.61%）. The extract showed moderate anti-bacterial activity with MIC values 100, 250, 125 mg/m L towards Escherichia coli, Staphylococcus aureus and Streptococcus pyogenus respectively. It exhibited high inhibition effect towards the fungi Candida albican with MFC value（250 mg/m L）. The extract had low antituberculosis activity with MIC value（100 mg/m L） and comparable MIC value（0.29 mg/m L） towards Plasmodium flaciparum.Conclusions: Supercritical CO2 extraction as alternate and green technology is performed successfully to extract the bioactive compounds from the seeds of T. foenum graecum Linn and it is concluded that this extract can be used as an alternate source of synthetic anti-biotic drugs.
This work evaluates the
antioxidant and antidiabetic activities of two metformin hydrochloride-based Schiff bases. Moreover, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) ...assay was used to examine the
cytotoxic effects of HL1 and HL2 on the A549 lung cancer cell line. The two Schiff bases that have been previously synthesized by using two effective, green techniques, namely stirring and microwave-assisted, are
-dimethyl-
′-(
)-(2-nitrophenyl) methylidene imidodicarbonimidic diamide and
-dimethyl-
′-(
)-(4-nitrophenyl) methylidene imidodicarbonimidic diamide, indicated by HL1 and HL2, respectively. Studies of antidiabetic efficacy using alpha-amylase revealed that HL2 has a higher inhibition than HL1, but the results on sucrase enzyme showed that HL1 had the highest inhibitory action, whereas the outcome of the antioxidant test with the 2,2-diphenyl-1-picrylhydrazyl assay demonstrated that HL2 was the most effective antioxidant, followed by ascorbic acid and HL1. In the MTT assay, HL1 had the best result, with an IC
value of 57.13 µg/mL compared to HL2 with an IC
value of 76.83 µg/mL. It was observed that HL1 was the most effective against the human lung cancer cell line A459. The findings were supported by computational and pharmacokinetic studies (SwissADME). Based on empirical and computational studies, we suggest that HL1 and HL2 are promising candidates as antioxidants and antidiabetics after being examined
A series of novel compounds, mono-5-isoxazolidines, and bis (5-isoxazolidines) derivatives, were prepared as bicycloadducts. The new series of isoxazolidines were designed and synthesized via ...1,3-dipolar cycloaddition reaction of nitrones with 3,9-Divinyl-2,4,8,10-tetra oxaspiro (5-5) undecane in the context of new antimicrobial and antioxidant drugs discovery and were fully characterized by FT-IR, 13C-NMR, and 1H-NMR spectroscopy. The physicochemical properties of all the novel cycloadducts, like bioactivity score and lipophilicity, were predicted using calculative methods. Similarly, the pharmacokinetic properties such as metabolism, absorption, distribution, and excretion (ADME) were also predicted. Most of the tested compounds exhibited antimicrobial properties to varying degrees against various bacterial species, including the Gram-negative bacteria Pseudomonas aeruginosa and Escherichia coli, and the Gram-positive bacteria Streptococcus pyogenus and Staphylococcus aureus, Antifungal properties were also observed against the tested fungi like Candida albicans, Aspergillus niger, and Aspergillus clavatus. The activity data exhibited that most compounds have high activity as compared to the standard drugs. In the range of graded doses, the results of some selected compounds revealed that some are high antioxidants while others are moderate or weak antioxidants. As evidenced by the molecular docking studies, the synthesized compounds showed good binding mode better than a standard drug, against the protein of a Pantothenate Synthetase enzyme (PDB-2X3F).
Isoxazolidines; Bicycloadducts; Nitrones; 1,3-Dipolar cycloaddition reaction.; Drug-likeness; Docking study.
The impact of the trace quantity of water into the ionic liquid (IL) was investigated for the synthesis of highly substituted pyridine by the one pot three component condensation of aldehyde, ...malononitrile and thiophenol at reflux temperature. Water shown much more dramatic acceleration effect on the catalytic activity of choline hydroxide (ChOH) by diffusion of ions. This novel methodology describes the formation of the micro-heterogenous component by water depleted IL media. The present protocol offers a formation of new C-C and C-S bond, undoubtedly point out the task and recyclability of choline hydroxide.
Celotno besedilo
Dostopno za:
BFBNIB, DOBA, GIS, IJS, IZUM, KILJ, KISLJ, NUK, PILJ, PNG, SAZU, UILJ, UKNU, UL, UM, UPUK
This study sought to assess the heavy metal content, phytochemical composition, antibacterial activity, and absorption, distribution, metabolism, and excretion (ADME) properties of
L. tree. The heavy ...metal content of the plant roots was determined using inductively coupled plasma-mass spectrometry technique, and it was found that only Cr, Mn, Fe, and Ni concentrations were above the permissible limits for edible plants. Gas chromatography-mass spectrometry analysis identified 11 phytochemicals in the aqueous extract of the plant. Both
and
confirmed the extract’s antibacterial efficacy. The aqueous extract showed significant antibacterial activity, with minimal inhibition concentration values of 125 µg/mL against
,
, and
. Among the 11 identified compounds, 1,8-Dioxa-5-thiaoctane,8-(9-borabicyclo3,3,1non-9-yl)-3-(9 borabicyclo3,3,1non-9-yloxy)-1-phenyl- showed the highest docking score (−8.31 kcal/mol) when docked into the active site of
MenB protein (PDB id: 3t88). It formed four hydrogen bonds with GLY86, GLY85, GLY132, and GLY133. Furthermore, the identified compounds were analyzed for ADME properties, most of them showed very good pharmacokinetic properties and did not violate Lipinski’s Rule of Five. Additional research is required to determine the medicinal potential of the compounds that have antibacterial activity.
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