Multiple molecular targets mediated antioxidant activity, molecular docking, ADMET, QSAR and bioactivity studies of halo substituted urea derivatives of α-Methyl-l-DOPA.

A series of novel α-methyl-l-DOPA urea derivatives viz., 3-(3,4-dihydroxyphenyl)-2-methyl-2-(3-halo/trifluoromethyl substituted phenyl ureido)propanoic acids (6a-e) have been synthesized from the reaction of α-methyl-l-DOPA (3) with various aryl isocyanates (4a-e) by using triethylamine (5, TEA) as a base catalyst in THF at reflux conditions. The synthesized compounds are structurally characterized by spectral (IR, H &C NMR and MASS) and elemental analysis studies and screened for their in-vitro antioxidant activity against DPPH, NO and HO free radical scavenging assays and identified compounds 6c &6d as potential antioxidants.

A Sensitive HPTLC Method for the Estimation of Glibenclamide, Rosiglitazone Maleate and Metformin Hydrochloride from a Multicomponent Dosage Form.

A sensitive, rapid and cost-effective method based on HPTLC with UV detection was developed for the quantitation of Glibenclamide (GLIBEN), Rosiglitazone maleate (ROSI) and Metformin hydrochloride (MET) from a combined dosage form. Pre-coated RP-18 F254s aluminum sheets were used as the stationary phase. Methanol-tetrahydrofuran-water-glacial acetic acid (16: 3.

Micelles entrapped microparticles technology: a novel approach to resolve dissolution and bioavailability problems of poorly water soluble drugs.

Aim of this study was to design a solid oral delivery system for a weakly basic drug such as dasatinib (DAS), so as to achieve pH-independent dissolution and improved oral bioavailability. DAS was solubilised using sodium lauryl sulphate as an aqueous micellar system and such a system containing lactose monohydrate as carrier was spray-dried to obtain a solid mass. Subsequently, the DAS-solid was converted into a tablet using conventional tableting methods.

Hunig's base catalyzed synthesis of new 1-(2,3-dihydro-1H-inden-1-yl)-3-aryl urea/thiourea derivatives as potent antioxidants and 2HCK enzyme growth inhibitors.

A series of 1-(2,3-dihydro-1H-indan-1-yl)-3-aryl urea/thiourea derivatives (4a-j) have been synthesized from the reaction of 2,3-dihydro-1H-inden-1-amine (2) with various aryl isocyanates/isothiocyanates (3a-j) by using N,N-DIPEA base (Hunig's base) catalyst in THF at reflux conditions. All of them are structurally confirmed by spectral (IR, H &C NMR and MASS) and elemental analysis and screened for their in-vitro antioxidant activity against DPPH and NO free radicals and found that compounds 4b, 4i, 4h &4g are potential antioxidants. The obtained in vitro results were compared with the molecular docking, ADMET, QSAR and bioactivity study results performed for them and identified that the recorded in silico binding affinities were observed in good correlation with the in vitro antioxidant results.

Taxogenomics Resolves Conflict in the Genus : A Two and Half Decades Pending Thought to Reclassify the Genus .

The genus is taxonomically well studied, and some members are model organisms. However, this genus is comprised of a heterogeneous group of members. 16S rRNA gene-based phylogeny of the genus indicates a motley assemblage of anoxygenic phototrophic bacteria (genus ) with interspersing members of other genera (chemotrophs) making the genus polyphyletic.

Separation of Unprecedented Degradants of Domperidone by Ultra-Performance Convergence Chromatography and Their Structure Elucidation.

Domperidone, a gastroprokinetic agent, is a common drug to treat emesis. It was subjected to acid, base-mediated hydrolysis, peroxide-mediated oxidation, photolysis and thermal degradation according to ICH guidelines to observe stability of the selected drug under the stress conditions. Although the drug is resistant to base hydrolysis, photolysis and thermal stressors, two degradants (DP-ISO1 and DP-ISO2) were formed in acid mediated hydrolysis.

Effect of Biohythane Production from Distillery Spent Wash with Addition of Landfill Leachate and Sewage Wastewater.

Rapid development of the industrial and domestic sectors has led to the rise of several energy and environmental issues. In accordance with sustainable development and waste minimization issues, biohydrogen production along with biomethane production via two-stage fermentation process using microorganisms from renewable sources has received considerable attention. In the present study, biohythane production with simultaneous wastewater treatment was studied in a two-stage (Biohydrogen and Biomethane) fermentation process under anaerobic conditions.

Relaxation dynamics of l-alanine in water medium investigated by dielectric relaxation spectroscopy.

The complex dielectric permittivity of L-alanine in aqueous medium at different concentrations and different temperatures were measured in the microwave (0.02 < ν/GHz < 20) frequency region by using open-ended coaxial probe technique. From the reflection coefficient and impedance data, the real and imaginary part of the dielectric permittivity values is determined.

Transdermal delivery of fluvastatin loaded nanoemulsion gel: Preparation, characterization and in vivo anti-osteoporosis activity.

The objective of present study was to develop hydrogel based nanoemulsion (NE) drug delivery system for transdermal delivery and evaluate its potential in in vivo anti-osteoporotic activity. NE was prepared using aqueous phase titration method and characterized for droplet size, zeta potential and morphology. It was then formulated into hydrogel based NE gel using carbopol 940 as gelling agent.

A novel pharmacological approach of herbal mediated cerium oxide and silver nanoparticles with improved biomedical activity in comparison with Lawsonia inermis.

Diabetes mellitus is one of the threatening, non-communicable and chronic ailments worldwide since ancient times to the current stage of human existence. The utilization of nanoparticles as a medicine in the treatment of diabetes is an attractive proposition. In the present study, herbal mediated cerium oxide nanoparticles (HMCeO NPs), herbal mediated silver nanoparticles (HMAg NPs) and Lawsonia intermix extract (LIE) was evaluated for them for in-vivo hypoglycemic effect and compared the potency.

Targeting PUMA/Bcl-xL interaction by new specific compounds to unleash apoptotic process in cancer cells.

We describe the first examples of small molecules able to disrupt the nanomolar interaction between the pro-apoptotic protein PUMA and its anti-apoptotic counterpart BcL-xL in malignant cells. Based on molecular modelling studies, we propose a rationale to this result, through a new "bottle-opener"-type strategy which could be of general use in the area of protein-protein interaction studies.

Bio oil production from microalgae via hydrothermal liquefaction technology under subcritical water conditions.

The upsurge in the concerning issues like global warming, environmental pollution and depletion of fossil fuel resources led to the thrust on third generation biofuels. Algal research has gained a lot of importance in the recent years. Effective utilization of algal biomass in a single step is necessary as it can produce Bio-oil (BO), gases and in addition to a variety of valuable products, along with nutrient recovery.

An AHP based optimized tuning of Modified Active Disturbance Rejection Control: An application to power system load frequency control problem.

This paper presents Modified Active Disturbance Rejection Control (MADRC) scheme and a systematic procedure to tune its tuning variables via. observer and controller gains. The problem of tuning is formulated as a constrained multi-objective optimization problem.

Fruit-Derived Polysaccharides and Terpenoids: Recent Update on the Gastroprotective Effects and Mechanisms.

Ulceration in the stomach develops in peptic ulcer disease when there is a loss of protective mucosal layers, particularly in infection. Antibiotic therapy has failed to eradicate and impede the colonization of . Despite given treatment, recurrent bleeding can occur and lead to death in the affected individual.

Monitoring and assessment of groundwater quality in a khondalitic terrain, Andhra Pradesh, India.

The groundwater quality assessment for the drinking and irrigation purpose is carried out in the Kandivalasa River Sub Basin covered with khondalitic suite (Garneti ferrous, Sillimanite, Gneiss) of rocks, near Cheepurupalli town of Vizianagaram district, Andhra Pradesh, India. The analysis for the groundwater quality for drinking has shown the slightly alkaline nature and high values of alkalinity in the study area. A very high concentration of total dissolved solids value is observed at one pocket where there has been contamination by many fertilizer industries located nearby the study area.

Non-enzymatic sensing of glucose using screen-printed electrode modified with novel synthesized CeO@CuO core shell nanostructure.

We fabricated a fourth generation glucose biosensor using CeO@CuO core shell nano structure (CeCCS NSs). A simple leave extract of Ocimum tenuiflorum was used to prepare different wt% of 0.2, 04, 0.

Novel drug targets for Mycobacterium tuberculosis: 2-heterostyrylbenzimidazoles as inhibitors of cell wall protein synthesis.

Background: Multi drug-resistant and mycobacterial infections are a major public health challenge, leading to high mortality and socioeconomic burdens through worldwide. Novel therapeutics are necessary to treat the drug resistant strains, since no new chemical entities are emerged in the last four decades for the treatment of TB.

Findings: A series of novel 2-heterostyrylbenzimidazole derivatives were synthesised by cyclisation of (3,4-diaminophenyl)(phenyl)methanone, cinnamic acid using glycerol in high yield.

User-Friendly HPLC Method Development and Validation for Determination of Enalapril Maleate and Its Impurities in Enalapril Tablets.

The official method for the determination of Enalapril Maleate and its related substances in European Pharmacopoeia (EP) is a gradient liquid chromatographic method. The method used styrene-divinylbenzene copolymer column, mobile phase buffer pH 6.8 and column oven temperature 70°C.

Molecular Modeling Studies of Novel Fluoroquinolone Molecules.

Background: Fluoroquinolones have been the centre of considerable scientific and clinical interest due to their broad spectrum pharmacological activities. Pefloxacin is an analogue of norfloxacin, which is a 3rd generation of fluoroquinolone antibiotic similar to ciprofloxacin. Pefloxacin is used to treat a variety of bacterial infections like respiratory tract, ear, nose and throat (ENT) infections, skin infections, and urinary tract infections.

Biosynthesis of MgO nanoparticles using mushroom extract: effect on peanut () seed germination.

Current study describes the green, environmental friendly, and cost-effectiveness technique for the preparation of MgO nanoparticles (NPs) via white button mushroom aqueous extract. The synthesized MgO NPs were characterized using equipments such as X-ray diffraction, dynamic light scattering (DLS), scanning electron microscope (SEM), energy dispersive spectroscopy (EDS), and thermal gravimetric analysis (TGA) for average crystalline size, particle size, morphology, elemental analysis, and weight loss of the materials, respectively. This study reports the application of gardened sizes of (20, 18.

Enhanced antimicrobial and anticancer properties of ZnO and TiO nanocomposites.

The study describes the antibacterial and anticancer activities of a nanocomposite prepared by mixing zinc oxide and titanium dioxide nanoparticles. The particle mixtures were analyzed by X-ray diffraction, Field emission scanning electron microscopy, transmission electron microscopy, Fourier transform infrared spectroscopy, and dynamic light scattering techniques. Thus, analyzed samples were subject to disc diffusion method at various concentrations to analyze their antibacterial activities against two Gram-positive and two Gram-negative bacteria.

Novel synthesis and characterization of pristine Cu nanoparticles for the non-enzymatic glucose biosensor.

Non enzymatic electrochemical glucose sensing was developed based on pristine Cu Nanopartilces (NPs)/Glassy Carbon Electrode (GCE) which can be accomplished by simple green method via ocimum tenuiflorum leaf extract. Then, the affect of leaf extract addition on improving Structural, Optical and electrochemical properties of pristine cu NPs was investigated. The synthesized Cu NPs were characterized with X-ray diffraction (X-ray), Uv-Visible spectroscopy (Uv-Vis), Fourier transformation infrared spectroscopy (FTIR), Particle size distribution (PSA), Scanning electron microscopy (SEM), Energy dispersive X-ray spectroscopy (EDS), Transmission electron microscopy (TEM) for structural optical and morphological studies respectively.

FLAVONOIDS AND ANTI-OXIDANT ACTIVITY MEDIATED GASTROPROTECTIVE ACTION OF LEATHERY MURDAH, TERMINALIA CORIACEA (ROXB.) WIGHT & ARN. LEAF METHANOLIC EXTRACT IN RATS.

Background: Leathery Murdah, Terminalia coriacea (Roxb.) Wight & Arn. from family Combretaceae is used in Ayurveda and Siddha traditional systems of medicine to heal ulcers.

CT- and MRI-based gross target volume comparison in vestibular schwannomas.

Aim: This study represents an enumeration and comparison of gross target volumes (GTV) as delineated independently on contrast-enhanced computed tomography (CT) and T1 and T2 weighted magnetic resonance imaging (MRI) in vestibular schwannomas (VS).

Background: Multiple imaging in radiotherapy improves target localization.

Methods And Materials: 42 patients of VS were considered for this prospective study with one patient showing bilateral tumor.