The cobalt(II), copper(II) and zinc(II) complexes of 1,10-phenanthroline (phen) and maltol (mal) (complexes 1, 2, 3 respectively) were prepared from their respective metal(II) chlorides and were characterized by FT-IR, elemental analysis, UV spectroscopy, molar conductivity, p-nitrosodimethylaniline assay and mass spectrometry. The X-ray structure of a single crystal of the zinc(II) analogue reveals a square pyramidal structure with distinctly shorter apical chloride bond. All complexes were evaluated for their anticancer property on breast cancer cell lines MCF-7 and MDA-MB-231, and normal cell line MCF-10A, using (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and morphological studies. Complex 2 was most potent for 24, 48 and 72 h treatment of cancer cells but it was not selective towards cancer over normal cells. The mechanistic studies of the cobalt(II) complex 1 involved apoptosis assay, cell cycle analysis, dichloro-dihydro-fluorescein diacetate assay, intracellular reactive oxygen species assay and proteasome inhibition assay. Complex 1 induced low apoptosis, generated low level of ROS and did not inhibit proteasome in normal cells. The study of the DNA binding and nucleolytic properties of complexes 1-3 in the absence or presence of H2O2 or sodium ascorbate revealed that only complex 1 was not nucleolytic.
The synthesis and characterization of two cobalt(II) complexes, Co(phen)(ma)Cl 1 and Co(ma)(2)(phen) 2, (phen=1,10-phenanthroline, ma(-)=maltolate or 2-methyl-4-oxo-4H-pyran-3-olate) are reported herein. The complexes have been characterized by FTIR, CHN analysis, fluorescence spectroscopy, UV-visible spectroscopy, conductivity measurement and X-ray crystallography. The number of chelated maltolate ligands seems to influence their DNA recognition, topoisomerase I inhibition and antiproliferative properties.
The drug resistance phenomenon in microbes is resulting in the ineffectiveness of available drugs to treat the infections. Thus, there is a continued need to discover new molecules to combat the drug resistance phenomenon. Norfloxacin is a fluoroquinolone antibiotic that is used for the treatment of urinary tract infections. In this research work, norfloxacin is structurally modified by hybridizing with a range of substituted acetohydrazidic moieties through a multistep reaction. The first step involves the coupling of norfloxacin 1 with methyl chloroacetate followed by the treatment with hydrazine hydrate to result in corresponding acetohydrazide 3. A range of substituted benzaldehydes were reacted with the acetohydrazide to form the targeted series of norfloxacin derivatives 4a-i. The final compounds were screened for antimicrobial activity. Among the tested compounds, 4c, 4d, 4e and 4f displayed better antifungal activity against F.avenaceum, while compound 4c and 4e were active against F. bubigeum.
We report the synthesis and biological evaluation of two new series of 2-amino-6-benzyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides and 2-amino-6-methyl-4-phenyl-4,6-dihydrobenzo[c]pyrano[2,3-e][1,2]thiazine-3‑carbonitrile 5,5-dioxides. The synthetic methodology involves a multistep reaction starting with methyl anthranilate which was coupled with methane sulfonyl chloride. The product of the reaction was subjected to N-benzylation and N-methylation reactions followed by ring closure with sodium hydride resulting in the formation of respective 2,1-benzothiazine 2,2-dioxides. These 2,1-benzothiazine precursors were subjected to multicomponent reaction with malononitrile and substituted benzaldehydes for the synthesis of two new series of pyranobenzothiazines (6a-r and 7a-r). The synthesized compounds were screened as selective inhibitors of monoamine oxidase A and monoamine oxidase B. The in vitro results suggested that compound 6d and 7q are the selective inhibitors of monoamine oxidase A, however, the selective and potent inhibitors of monoamine oxidase B included compounds 6h and 7r. Moreover, some dual inhibitors were noticed like 7l having more inhibitory activity towards both the isozymes. Moreover, the binding modes of the selective and potent inhibitors of monoamine oxidase A and B were investigated by molecular docking analysis. The results suggested that the synthetic derivatives may be potential towards the monoamine oxidase isozymes.
The aim of this research was to synthesize and develop a new method for the preparation of iron oxide (Fe(3)O(4)) nanoparticles on talc layers using an environmentally friendly process. The Fe(3)O(4) magnetic nanoparticles were synthesized using the chemical co-precipitation method on the exterior surface layer of talc mineral as a solid substrate. Ferric chloride, ferrous chloride, and sodium hydroxide were used as the Fe(3)O(4) precursor and reducing agent in talc. The talc was suspended in deionized water, and then ferrous and ferric ions were added to this solution and stirred. After the absorption of ions on the exterior surface of talc layers, the ions were reduced with sodium hydroxide. The reaction was carried out under a nonoxidizing oxygen-free environment. There were not many changes in the interlamellar space limits (d-spacing = 0.94-0.93 nm); therefore, Fe(3)O(4) nanoparticles formed on the exterior surface of talc, with an average size of 1.95-2.59 nm in diameter. Nanoparticles were characterized using different methods, including powder X-ray diffraction, transmission electron microscopy, emission scanning electron microscopy, energy dispersive X-ray spectroscopy, and Fourier transform infrared spectroscopy. These talc/Fe(3)O(4) nanocomposites may have potential applications in the chemical and biological industries.
In this research, silver nanoparticles (AgNPs) were synthesized in chitosan (Cts), Cts/gelatin and gelatin suspensions using a chemical reducing agent. Cts and gelatin were used as natural stabilizers and solid support, whereas AgNO(3) was used as the silver precursor. Sodium borohydride (NaBH(4)) was used as the reducing agent. The properties of AgNPs in Cts, Cts/gelatin and gelatin bionanocomposites (BNCs) were studied in terms of their surface plasmon resonance, crystalline structure, average diameter size, particle distributions, surface topography and functional groups. All the samples were characterized by UV-visible spectroscopy, powder X-ray diffraction, transmission electron microscopy, atomic force microscopy and Fourier transform infrared spectroscopy.
The present study defines a novel green method for the synthesis of the nickel oxide nanocatalyst by using an aqueous latex extract of the Ficus elastic. The catalyst was examined for the conversion of novel Brachychiton populneus seed oil (BPSO) into biodiesel. The Brachychiton populneus seeds have a higher oil content (41 wt%) and free fatty acid value (3.8 mg KOH/g). The synthesised green nanocatalyst was examined by the Fourier transform infrared (FT-IR) spectroscopy, energy dispersive X-Ray (EDX) spectroscopy, X-Ray diffraction (XRD) spectroscopy and scanning electron microscopy (SEM). The obtained results show that the synthesised green nanocatalyst was 22-26 nm in diameter and spherical-cubic in shape with a higher rate of catalytic efficiency. It was utilised further for the conversion of BPSO into biofuel. Due to the high free fatty acid value, the biodiesel was synthesised by the two-step process, i.e., pretreatment of the BPSO by means of acid esterification and then followed by the transesterification reaction. The acidic catalyst (H2SO4) was used for the pretreatment of BPSO. The optimum condition for the transesterification of the pretreated BPSO was 1:9 of oil-methanol molar ratio, 2.5 wt % of prepared nanocatalyst concentration and 85 °C of reaction temperature corresponding to the highest biodiesel yield of 97.5 wt%. The synthesised biodiesel was analysed by the FT-IR and GC-MS technique to determine the chemical composition of fatty acid methyl esters. Fuel properties of Brachychiton populneus seed oil biodiesel (BPSOB) were also examined, compared, and it falls in the prescribed range of ASTM standards.
α-Glucosidase inhibitors occupy a prominent position among the various treatments of type-2 diabetes mellitus (DM2). In this study, a series of new norfloxacin-acetanilide hybrid molecules were synthesized and screened for α-glucosidase inhibition activity. The synthetic methodology involves the synthesis of a series of α-bromoacetanilides by condensing bromoacetyl bromide with various substituted anilines. These α-bromoacetanilides were coupled with norfloxacin in DMF to get the titled hybrids. The structure elucidation of synthesized compounds were characterized by 1H NMR, 13C NMR and LC-MS. Finally, the compounds were screened for their α-glucosidase inhibition activity using acarbose as a reference drug (IC50 =58 μM). Among the tested compounds, 3i and 3j displayed potent α-glucosidase inhibition activity with IC50 values of 7.81±0.038 and 5.55±0.012 μM respectively. In-addition, 3m, 3f and 3k were demonstrated moderate alpha-glucosidase inhibition activities with IC50 values of 52.905±0.041, 23.79± 0.087 and 23.06±0.026 μM respectively. The structure-activity relationship was established with the help of molecular docking by using Molecular Operating Environment software (MOE 2014).
Diabetes mellitus (DM) is a chronic disorder and has affected a large number of people worldwide. Insufficient insulin production causes an increase in blood glucose level that results in DM. To lower the blood glucose level, various drugs are employed that block the activity of the α-glucosidase enzyme, which is considered responsible for the breakdown of polysaccharides into monosaccharides leading to an increase in the intestinal blood glucose level. We have synthesized novel 2-(3-(benzoyl/4-bromobenzoyl)-4-hydroxy-1,1-dioxido-2H-benzo[e][1,2]thiazin-2-yl)-N-arylacetamides and have screened them for their in silico and in vitro α-glucosidase inhibition activity. The derivatives 11c, 12a, 12d, 12e, and 12g emerged as potent inhibitors of the α-glucosidase enzyme. These compounds exhibited good docking scores and excellent binding interactions with the selected residues (Asp203, Asp542, Asp327, His600, Arg526) during in silico screening. Similarly, these compounds also showed good in vitro α-glucosidase inhibitions with IC50 values of 30.65, 18.25, 20.76, 35.14, and 24.24 μM, respectively, which were better than the standard drug, acarbose (IC50 = 58.8 μM). Furthermore, a good agreement was observed between in silico and in vitro modes of study.
Silver nanoparticles (AgNPs) of a small size were successfully synthesized using the wet chemical reduction method into the lamellar space layer of montmorillonite/chitosan (MMT/Cts) as an organomodified mineral solid support in the absence of any heat treatment. AgNO3, MMT, Cts, and NaBH4 were used as the silver precursor, the solid support, the natural polymeric stabilizer, and the chemical reduction agent, respectively. MMT was suspended in aqueous AgNO3/Cts solution. The interlamellar space limits were changed (d-spacing = 1.24-1.54 nm); therefore, AgNPs formed on the interlayer and external surface of MMT/Cts with d-average = 6.28-9.84 nm diameter. Characterizations were done using different methods, ie, ultraviolet-visible spectroscopy, powder X-ray diffraction, transmission electron microscopy, scanning electron microscopy, energy dispersive X-ray fluorescence spectrometry, and Fourier transform infrared spectroscopy. Silver/montmorillonite/chitosan bionanocomposite (Ag/MMT/Cts BNC) systems were examined. The antibacterial activity of AgNPs in MMT/Cts was investigated against Gram-positive bacteria, ie, Staphylococcus aureus and methicillin-resistant S. aureus and Gram-negative bacteria, ie, Escherichia coli, E. coli O157:H7, and Pseudomonas aeruginosa by the disc diffusion method using Mueller Hinton agar at different sizes of AgNPs. All of the synthesized Ag/MMT/Cts BNCs were found to have high antibacterial activity. These results show that Ag/MMT/Cts BNCs can be useful in different biological research and biomedical applications, including surgical devices and drug delivery vehicles.
Small sized magnetite iron oxide nanoparticles (Fe3O4-NPs) with were successfully synthesized on the surface of rice straw using the quick precipitation method in the absence of any heat treatment. Ferric chloride (FeCl3·6H2O), ferrous chloride (FeCl2·4H2O), sodium hydroxide (NaOH) and urea (CH4N2O) were used as Fe3O4-NPs precursors, reducing agent and stabilizer, respectively. The rice straw fibers were dispersed in deionized water, and then urea was added to the suspension, after that ferric and ferrous chloride were added to this mixture and stirred. After the absorption of iron ions on the surface layer of the fibers, the ions were reduced with NaOH by a quick precipitation method. The reaction was carried out under N2 gas. The mean diameter and standard deviation of metal oxide NPs synthesized in rice straw/Fe3O4 nanocomposites (NCs) were 9.93 ± 2.42 nm. The prepared rice straw/Fe3O4-NCS were characterized using powder X-ray diffraction (PXRD), transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy dispersive X-ray fluorescence (EDXF) and Fourier transforms infrared spectroscopy (FT‒IR). The rice straw/Fe3O4-NCs prepared by this method have magnetic properties.
Urease, a nickel-dependent enzyme found in various life forms, catalyzes urea breakdown, concluding nitrogen metabolism by generating ammonia and carbamate. This process causes a rise in pH, supports the survival of pathogens, and can lead to infections such as gastric disorders like ulcers and cancer in humans. Helicobacter pylori employs urease for survival in the acidic environment of the stomach and in protein synthesis. To treat such infections and inhibit the growth of pathogens, it is mandatory to obstruct urease activity; therefore, derivatives of 1-(3-nitropyridin-2-yl)piperazine were synthesized (5a-o; 7a-k). All these newly synthesized compounds were investigated for urease inhibition by in vitro inhibition assays. The results showed that 5b and 7e are the most active inhibitors, having IC50 values of 2.0 ± 0.73 and 2.24 ± 1.63 µM, respectively. These IC50 values are lower than the IC50 value of the standard thiourea, which was 23.2 ± 11.0 µM. The hemolysis potential of 5b, 5c, 5i, 7e, and 7h was also determined; 7e and 7h exhibited good biocompatibility in human blood cells. Through in silico analysis, it was shown that both these potent inhibitors develop favorable interactions with the active site of urease, having binding energies of -8.0 (5b) and -8.1 (7e) kcal/mol. The binding energy of thiourea was -2.8 kcal/mol. Moreover, 5b and 7e have high gastrointestinal permeability as predicted via computational analysis. On the other hand, the IC50 value and binding energy of precursor compound 3 was 3.90 ± 1.91 µM and -6.1 kcal/mol, respectively. Consequently, 5b and 7e can serve as important inhibitors of urease.
Several borehole problems are encountered during drilling a well due to improper mud design. These problems are directly associated with the rheological and filtration properties of the fluid used during drilling. Thus, it is important to investigate the mud rheological and filtration characteristics of water-based drilling muds (WBMs). Several materials have been examined but due to the higher temperature conditions of wells, such materials have degraded and lost their primary functions. In this research, an attempt was made to prepare a water-based mud by utilizing graphene nano platelets (GNP) in addition to the native tapioca starch at different ratios. The combined effect of starch and graphene nano platelets has been investigated in terms of mud's rheological and filtration parameters, including its plastic viscosity (PV), yield point (YP), fluid loss volume (FLV) and filtercake thickness (FCT). The morphological changes in the filtercake have also been observed using Field Emission Scanning Electron Microscope (FESEM) micrographs. Plastic viscosity was increased from 18-35 cP, 22-31 cP and 21-28 cP for 68 °F, 250 °F and 300 °F, respectively. The yield point was also enhanced from 22-37 lb/100ft2, 26-41 lb/100ft2 and 24-31 lb/100ft2 at the studied range. The fluid loss was dramatically reduced from 14.5-6.5 mL, 17.3-7.5 mL and 36-9.5 mL at 68 °F, 250 °F and 300 °F respectively. Similarly, filtercake thickness was also reduced which was further illustrated by filtercake morphology.
Biochar/layered double hydroxide (LDH) composites have gained considerable attention in recent times as low-cost sustainable materials for applications in water treatment. This paper critically evaluates the latest development in applications of biochar/LDH composites in water treatment with an emphasis on adsorption and catalytic degradation of various pollutants. The adsorption of various noxious contaminants, i.e., heavy metals, dyes, anions, and pharmaceuticals onto biochar/LDH composites are described in detail by elaborating the adsorption mechanism and regeneration ability. The synergistic effect of LDH with biochar exhibited significant improvement in specific surface area, surface functional groups, structure heterogeneity, stability, and adsorption characteristics of the resulting biochar/LDH composites. The major hurdles and challenges associated with the synthesis and applications of biochar/LDH composites in water remediation are emphasized. Finally, a roadmap is suggested for future research to assure the effective applications of biochar/LDH composites in water purification.
The relative yields of ϒ mesons produced in pp and Pb-Pb collisions at sqrt[s_{NN}]=5.02 TeV and reconstructed via the dimuon decay channel are measured using data collected by the CMS experiment. Double ratios are formed by comparing the yields of the excited states, ϒ(2S) and ϒ(3S), to the ground state, ϒ(1S), in both Pb-Pb and pp collisions at the same center-of-mass energy. The double ratios, [ϒ(nS)/ϒ(1S)]_{Pb-Pb}/[ϒ(nS)/ϒ(1S)]_{pp}, are measured to be 0.308±0.055(stat)±0.019(syst) for the ϒ(2S) and less than 0.26 at 95% confidence level for the ϒ(3S). No significant ϒ(3S) signal is found in the Pb-Pb data. The double ratios are studied as a function of collision centrality, as well as ϒ transverse momentum and rapidity. No significant dependencies are observed.
The nuclear modification factor [Formula: see text] and the azimuthal anisotropy coefficient [Formula: see text] of prompt and nonprompt (i.e. those from decays of b hadrons) [Formula: see text] mesons, measured from PbPb and pp collisions at [Formula: see text] [Formula: see text] at the LHC, are reported. The results are presented in several event centrality intervals and several kinematic regions, for transverse momenta [Formula: see text] [Formula: see text] and rapidity [Formula: see text], extending down to [Formula: see text] [Formula: see text] in the [Formula: see text] range. The [Formula: see text] of prompt [Formula: see text] is found to be nonzero, but with no strong dependence on centrality, rapidity, or [Formula: see text] over the full kinematic range studied. The measured [Formula: see text] of nonprompt [Formula: see text] is consistent with zero. The [Formula: see text] of prompt [Formula: see text] exhibits a suppression that increases from peripheral to central collisions but does not vary strongly as a function of either y or [Formula: see text] in the fiducial range. The nonprompt [Formula: see text] [Formula: see text] shows a suppression which becomes stronger as rapidity or [Formula: see text] increases. The [Formula: see text] and [Formula: see text] of open and hidden charm, and of open charm and beauty, are compared.
A study of vector boson scattering in pp collisions at a center-of-mass energy of 8 TeV is presented. The data sample corresponds to an integrated luminosity of 19.4 fb(-1) collected with the CMS detector. Candidate events are selected with exactly two leptons of the same charge, two jets with large rapidity separation and high dijet mass, and moderate missing transverse energy. The signal region is expected to be dominated by electroweak same-sign W-boson pair production. The observation agrees with the standard model prediction. The observed significance is 2.0 standard deviations, where a significance of 3.1 standard deviations is expected based on the standard model. Cross section measurements for W(±)W(±) and WZ processes in the fiducial region are reported. Bounds on the structure of quartic vector-boson interactions are given in the framework of dimension-eight effective field theory operators, as well as limits on the production of doubly charged Higgs bosons.
Measurements of normalized differential cross sections as functions of the multiplicity and kinematic variables of charged-particle tracks from the underlying event in top quark and antiquark pair production are presented. The measurements are performed in proton-proton collisions at a center-of-mass energy of 13 Te , and are based on data collected by the CMS experiment at the LHC in 2016 corresponding to an integrated luminosity of 35.9 fb - 1 . Events containing one electron, one muon, and two jets from the hadronization and fragmentation of b quarks are used. These measurements characterize, for the first time, properties of the underlying event in top quark pair production and show no deviation from the universality hypothesis at energy scales typically above twice the top quark mass.
Events with no charged particles produced between the two leading jets are studied in proton-proton collisions at s = 7 TeV . The jets were required to have transverse momentum p T jet > 40 GeV and pseudorapidity 1.5 < | η jet | < 4.7 , and to have values of η jet with opposite signs. The data used for this study were collected with the CMS detector during low-luminosity running at the LHC, and correspond to an integrated luminosity of 8 pb - 1 . Events with no charged particles with p T > 0.2 GeV in the interval - 1 < η < 1 between the jets are observed in excess of calculations that assume no color-singlet exchange. The fraction of events with such a rapidity gap, amounting to 0.5-1% of the selected dijet sample, is measured as a function of the p T of the second-leading jet and of the rapidity separation between the jets. The data are compared to previous measurements at the Tevatron, and to perturbative quantum chromodynamics calculations based on the Balitsky-Fadin-Kuraev-Lipatov evolution equations, including different models of the non-perturbative gap survival probability.