Derpharmachemica

A new series of heterocyclic compounds containing both N-methyl thiotetrazole (NMTT) and piperidine nuclei together, namely ethyl 5-(1- methyl-1H-tetrazol-5-ylthio)-4-oxo-2,6-substituted diphenylpiperidine-3-caboxylate derivatives, were synthesized by cyclocondensation of ethyl 4-(1-methyl-1H-tetrazol-5-ylthio)-3-oxobutanoate with ammonium acetate and substituted aromatic aldehydes. The synthesized N-methylthiotetrazole substituted piperidine-4-one derivatives were evaluated for their antimicrobial activity using disc diffusion method. The structures of the synthesized compounds were characterized by Infrared Radiation (IR), Proton Nuclear Magnetic Resonance (1H-NMR), Carbon-13 (C13) Nuclear Magnetic Resonance (13C-NMR), 2D-NMR and mass spectral data. The antimicrobial activity reveals that several compounds exhibit good antibacterial activity when compared with the reference drug. Molecular docking studies were performed against malarial activities. 

The Safety of the stem bark of Acacia Siberian, as an antidiarrheal, in Albino rats (four groups) has not yet been evaluated. Thisstudy to identify the effect of the acetone extract of the stem bark of Acacia Siberian (AESBAS) on Albino rats, Separation andidentification of the acetone extract of the stem bark of Acacia Siberian by GC-MS-TMS analysis. Albino rats (four groups) were subjected to the sub-chronic oral administration of the AESBAS for Twenty-eight days. Phytochemical screening test of the AESBAS confirmed by GC-MS-TMS analysis. Non-significant effect (p>0.05) in mean weight gain during the end of the experiment between groups. Also, some hematological analysis in the twenty-ninth day was estimated using standard steps. The AESBAS had non-significant effect (p>0.05) on some hematological analysis on study groups compared with the control group, that were given varying doses of the AESBAS. The components of AESBAS confirmed by GC-MS-TMS analysis. The results of this ...

Polycyclic Aromatic Hydrocarbons (PAHs) are a series of organic contaminants that have become ubiquitous in the environment. For the general population, exposures of humans to environmental pollutants, such as PAHs, can occur by various pathways, such as drinking water, inhalation of ambient air and ingestion of food (e.g., seafood). The exposure to high concentrations of PAHs together with other factors couldcontribute to the decreased health of fish living in marine ecosystem and the assessment of the impact on biota is of considerable concern. The aim of the present research was to study the bioaccumulation of four selected PAH in Sardina pilchardus collected from ten locations along the Moroccan coasts. PAHs determinations were performed using Gas chromatography-mass spectroscopy (GC/MS). The carcinogenic toxicity (TEQBaP), exposure daily intake (EDI), margin of exposure (MOE) and excess cancer rate (ECR) of four priority PAHs were evaluated. The results of this study have confir...

A new series of 4-methyl-7-triazolylmethoxy-2H-benzopyran-2-ones were synthesized using 7-hydroxy-4-methyl-2H-benzopyran-2-one as the starting material. It was first converted into 7-yloxyacetohydrazide by functional group inter conversion strategies and then reacted with aromatic or heterocyclic aldehydes and ammonium acetate in acetic acid to give the titled compounds. All the synthesized compounds wereevaluated for their in vitro antibacterial and antifungal activities against seven strains of bacteria and four strains of fungi. MIC results of most of the synthesized compounds (14-23, 26-27 and 29) have shown them to possess promising to comparable activities while compounds 15, 19, 21, 26, 27 and 29 were found to be better antifungal agents than the standard drugs in vitro and can serve as lead molecules to discover a new antimicrobial in future to combat the growing drug resistance and infections developed by various microorganisms. 

A single step process for the synthesis of quinoline-3-carboxylic acid was developed from 2’-amino acetophenons. With this method a Key intermediate of ciprofloxacin is prepared.

Benzimidazole is a very stable nucleus and the derivatives of 2-methyl benzimidazole may show different and better biological activity. Thepresence of the thiazolidinone ring in a benzimidazole derivative enhances its antimicrobial activity. 2-methyl benzimidazole derivative are formed by the condensation of o-phenylenediamine with acetic acid. Combination of two or more active moieties into one is a common procedure, can result in augmenting the activity and removes untoward side effects. Hence, the present work focuses on synthesis of potent antimicrobial benzimidazole derivatives by the condensation of Schiff's bases of 2-methyl benzimidazole moiety with thiomalic acid affording the thiazolidinone ring and to study their antimicrobial activity. In antibacterial activity (Staphylococcus aureus and Escherichia coli), it shows that compound TE6 is the most active compound and in antifungal activity (Candida albicans), TE3 & TE4 are found to be most active.

The variation in the Physico Chemical properties of Beta Asarone when the temperature is raised is studied here. The Solvent effect has alsobeen calculated with 2 solvents-water and ethanol by (Polarizable continuum Model (PCM) method where a solute cavity is created by a set ofover lapping spheres and computes the energy in solution. The electrostatic interactions of molecules are studied using their Mulliken charge distribution. SCF Energy, Molecular electrostatic Potential mapping, Dipole moment, Ionization Potential and Thermal properties are also studied. Beta Asarone which is the reported toxic constituent of Acorus calamus might undergo variations with higher temperature and also when it is in solution. The study of variations in solution is challenging and here the quantum mechanical calculations are performed in two different solutions to test for any variations of Beta Asarone in solution.

Several theoretical approachs could not define clearly the strong local attacks between the electrophilic and nucleophilic reagent when the local attack was predicted in the various methodologies, the various solvents and by the various substituents of reagents. For this, we have proposed anew descriptor, named ΔZ. Indeed, when ∆Z difference is very weaker, the local interaction is very strong and vice versa. This descriptor serves to select the best methodology, the best solvent or the possible geometries of reagents. This descriptor has been succefully evaluated. 

A simple, low cost and highly sensitive catalytic hydrogen signals (CHSs) technique has established for the investigation of Manganese(II) by means of ammonium 4-phenylpiperazine-1-dithiocarbamate and ammonium 4-benzylpiperidine-1-dithiocarbamate in various ecofriendly and biological matrices using D.C. polarography. This procedure was initiated on the reaction of Manganese (II) in APP-DTC/ABP-DTC in the existence of NH4Cl-NH4OH medium at pH 6.6 and 7.2 respectively. The resulting oxidation signals were obtained at -0.78 V and -0.64 V vs SCE, owing to the CHSs. Different experimental conditions such as pH effects, background electrolyte (NH4Cl-NH4OH) effects and DTCs and Manganese(II) ion effects have been studied. The current procedure was effectively applied for the testing of Manganese(II) in sundry environmental and biological samples and attained recovery percentages (95-99%) are comparable to the Atomic Absorption Spectrophotometry (AAS) method. 

An efficient and convenient approach for the synthesis of diaryl ethers via the one-pot synthesis of and aryl boronic acids and phenols in the presence of copper acetate and 2,2'-bipyridine under ultrasonic irradiation. This procedure has high conversions with good product yields, less reaction time, gainful cost, air stable, easy purification, and environmentally benign reaction conditions. All synthesized compounds were characterized by spectral techniques, like Proton Nuclear Magnetic Resonance (1H-NMR), Carbon-13 Nuclear Magnetic Resonance (13C-NMR) and Mass Spectrometry (MS). 

A novel series of five 7-piperazin-substituted [1,3]oxazolo[4,5-d]pyrimidines have been synthesized and characterized by Infrared (IR), Proton Nuclear Magnetic Resonance ( 1H-NMR), Carbon-13 Nuclear Magnetic Resonance (13C-NMR) spectroscopy, elemental analysis and chromatomass-spectrometry. The anticancer activities of the all the newly synthesized compounds were valuated via single high dose (10-5M) against 60 cancer cell lines by the National Cancer Institute according to its own screening protocol. In the next phase, the compounds have been selected for five-dose assay. Among these compounds 5-phenyl-7-piperazin-1-yl-2-p-tolyl[1,3]oxazolo[4,5-d]pyrimidine displayed the most growth inhibitory (GI50 was in range of 0.22.0 μM), cytostatic (TGI  0.3-4.2 μM) and cytotoxic (LC50  0.6-7.8 μM with the exception of Leukemia CCRF-CEM cell line, LC50>100 μM) activities against all cancer cell lines. The most selectivity 5-phenyl-7-piperazin-1-yl-2-ptolyl[1,3]oxazolo[4,5-d]pyrimidine d...

Penicillium purpurogenum, order Eurotiales was a superior producer to red, orange and yellow colorants. The fungus was grown in Dox media, it was found that Mannitol (30 g/l) and peptone (4 g/l) doubled the fungal productivity more than fourteen folds. The optimum conditions forpigment production was found to be at faint alkaline media (pH 8) at ambient temperature (30oC), at which a sharp increase of pigment yield was attained (263.63 g/l). During fermentation, the fungus was subjected to physical stress; Viz. high and low temperatures, magnetic field, and different wave lengths of light. The microorganism maintained its activity at the aforementioned physical effects. 

Novel Chalcones is considered as an important chemical for the synthesis of various physiological significance and pharmacological utilized molecules. Traditionally, chalcones are prepared by Claisen-Schmidt condensation. The structures of the newly synthesized compounds (3a-3o)were elucidated by Infrared (IR), Proton Nuclear Magnetic Resonance (1H-NMR), Mass spectroscopy. All the synthesized compounds (3a-3o) screened for their anti-fungal activity and QSAR analysis was applied to a data set of 15 obtained Novel Chalcones derivatives and the best model described a strongly correlation between the anti-fungal activity and molecular descriptors as refractivity (MR), Ovality, HOMO energy (HE), LUMO energy (LE), partition coefficient (CLogP, LogP, Connolly accessible area (CAA), Connolly molecular area (CMA), Connolly solvent excluded area (CSEV). All the parameters showed significant correlation with biological activity (r<0.8), but the molar refractivity exhibited best correlation ...

Aims: The study refers to application of a synthetic candidate containing an indole scaffold, 5f, in animal models of behavioral despair. Moreover, binding affinity and polarizability of 5f were calculated with molecular docking and density functional theory (DFT) study, respectively. Materials and Methods: To compare, desipramine (DMI) (10 mg/kg, i.p.), a selective serotonin-norepinephrine reuptake inhibitor(SNRI) and fluoxetine (FLX) (10 mg/kg, i.p.), a selective serotonin reuptake inhibitor (SSRI) were employed. The binding affinity of 5f, FLX and DMI to LeuTa, a leucine tranporter as a homologous protein to monoamine, were evaluated. Also, polarizability of 5f was compared using DFT method. The neuroprotective effect of 5f on behavioral despair was evaluated using forced-swim and tail suspension tests in male mice. The drugs were injected intraperitoneally (i.p.) 30 minutes before the tests. Results: 5f (2.5, 5, 10 mg/kg) significantly reduced the immobility behavior in a dose-d...

The present study was undertaken to obtain Quantitative structure activity relationship (QSAR) models for predicting the antimicrobial activity of di-(alkyl/aryl)-substituted Tin (IV) metal complexes derived from Schiff bases of pyridoxal. A data set consisting of 12 di-(alkyl/aryl)- substituted Tin (IV) metal complexes derived from Schiff bases of pyridoxal was subjected to linear free energy regression analysis and QSARmodels were obtained for the respective microorganisms. The QSAR analysis revealed that energy of lowest unoccupied molecular orbital (LUMO), valence zero order molecular connectivity index (0  v ) and second order molecular connectivity index (2 ) were effectively moderating the antimicrobial activity of di-(alkyl/aryl)-substituted Tin (IV) metal complexes. The derived QSAR models have got excellent predictive power associated with them as evidenced by the low residual values. These models can be utilized for the prediction of antimicrobial activity of similar ty...

A simple, precise, linear stability indicating RP-HPLC method was developed and validated as per ICH guidelines for the determination of lamotrigine in the bulk drug and tablet dosage form. Chromatographic separation was performed by using agilant HPLC 1200 series includeisocratic mode on a C18 Qualisil BDS (250 mm × 4.5 mm × 5 mm) column using mobile phase containing potassium dihydrogen orthophosphate buffer (pH 7.4) and methanol in the ratio 60: 40 at flow rate 1.3 ml/min. The wavelength for detection was 305 nm at roomtemperature. The retention time for separation was 5.3 min and linearity of lamotrigine was perceived in the concentration range of 5-30 μg/ml with correlation coefficient of 0.999. Force degradation of lamotrigine was completed under acidic, basic, oxidation, dry heat and photolytic conditions. The method was found precise, linear, and accurate as per ICH guidelines and may be used as an alternative method in industry.

Nine biologically important pyrimidine derivatives have been prepared by conventional method and UV-irradiation methods. The percentage yield of a product was substantially higher (40%-88%) by UV-irradiation method compared to that (18%-51%) by conventional method. Moreover, the UV-irradiation method is an environmentally friendly method and avoids the pollution problem in organic synthesis. Thestructures of the compounds were verified by microanalysis (CHN), Infrared (IR) and Proton Nuclear Magnetic Resonance (1H-NMR)spectroscopies and X-ray powder diffraction analysis. The investigated compounds consist of a pyrimidine ring and two benzene rings with intermolecular N–H---N interaction between the adjacent molecules. The compounds crystallized in the monoclinic space group P-1. The synthesized products have also been tested for their anti-bacterial/anti-fungal and anti-oxidant activities. The compounds have shown comparatively higher activities against the fungal microbes as compare...

A series of new 5,5’ -(1-(aryl)-1H-pyrazole-3,4-diyl)bis-(2-aryl-1,3,4-oxadiazole) derivatives were synthesized by the condensation of 1-(aryl)- 1H-pyrazol-3,4-dicarbohydrazide with substituted aromatic acids. All the newly synthesized compounds were screened for their in vitroantibacterial and antioxidant activity. Among the tested compounds, bis-1,3,4-oxadiazole 3p exhibited excellent antioxidant activity. The structures of the newly synthesized compounds were confirmed by Proton Nuclear Magnetic Resonance (1H-NMR), InfraRed (IR), Liquid Chromatography-Mass Spectrometry (LC-MS), X-Ray Diffraction (XRD) and elemental analysis.

The inhibition of corrosion of mild steel in hydrochloric acid in the presence of Gnetum gnemon L. peel extract (GGPE) has been studied using the weight loss, potentiodynamic polarization, FTIR and scanning electron microscopy (SEM) analysis. It was found that the inhibition efficiency increased with increasing concentration of GGPE and temperature. The inhibition was assumed to occur via adsorption of inhibitor molecules on the metal surface. The adsorption of the extract on the mild steel is found to obey Langmuir adsorption isotherm and acts as a mixed-type inhibitor. Thermodynamic and kinetic parameter data for the adsorption process were calculated and discussed.

Two simple, precise, accurate and sensitive visible spectrophotometric methods (I and II) have been established for quantifying ribavirin in pure form and pharmaceutical preparations. The proposed method I is based on the ability of ribavirin to reduce Folin-Ciocalteau reagent in alkaline medium to form a highly stable blue colored complex that can be measured spectrophotometrically at 760 nm. Method II is based on the formation of colored stable charge transfer complex, measured spectrophotometrically at 550 nm, between dichloro-5,6-dicyano-1,4- benzoquinone and ribavirin in acetonitrile medium. Variables affecting the chemical reaction were studied and optimized. The suggested methods I and II were validated as per ICH guidelines and successfully applied for quantification of the ribavirin in its pharmaceutical preparations like tablets, capsules and injections dosage forms with good accuracy and precision.

2-(3-Methyl-4,5-dihydro-1H-1,2,4-triazol-5-on-4-yl)-azomethine)-benzoic acid has been optimized using B3LYP/6-31G(d) and HF/6-31G(d) basis sets. Thus, the most stable geometrical comformer of compound was obtained. Proton Nuclear Magnetic Resonance (1H-NMR) and Carbon-13 Nuclear magnetic Resonance (13C-NMR) spectral values according to GIAO method was calculated using Gaussian G09W program package in gas phase and in DMSO solvent. Theoretical and experimental values were plotted according to δ exp=a+b.d calc. Theoretical spectral values of molecule were calculated and compared with experimental values. The veda4f program was used in defining Infrared (IR) data. The standard error values were found via the Sigma plot with regression coefficient of a and b constants. The vibrational frequency values of this molecule have been calculated by using 6-31G (d) basis set with DFT and HF methods. Then, these values are multiplied with appropriate adjustment factors. In addition, the, thermody...

Schinus molle L. (Family: Anacardiaceae), also known by the Pepper tree (in English) and Qundo berbere (in Amargna). American/ Peruvian pepper is an evergreen tree of culinary and has medicinal importance. It’s essential oil (EO) has proven bioactivities. The aim of this study was to determine chemical composition of essential oil of leaves of S. molle growing in Haramaya University (HU) Main Campus (Dire Dawa, Ethiopia). Material and Method: Fresh leaves from S. molle were randomly collected from the plants growing in Haramaya University (Main Campus) was used to hydrodistillation with Clevenger apparatus to obtain essential oils. Gas chromatography mass spectrometry (GCMS) was used to determine chemical composition of essential oil. Result: Result from GC-MS suggested forty nine volatile components in which, limonene (18.23%), elemol (12.75%) &α-phellandrene (10.40%), α-pinene (6.51%), p-cymene (6.7%) & spathulenol (5.52%) were the major compounds. Conclusion: Comparison wi...

About nine 4-methoxyphenyl enones were synthesized by microwave assisted Crossed-Aldol condensation of 4-methoxyacetophenone and substituted benzaldehydes in the presence of FeCl3 /Bentonite catalyst under microwave irradiation. These enones were characterized by meltingpoints, micro analysis and spectroscopic data. The antimicrobial potential of these enones was tested by Bauer-Kirby disc diffusion method. Many of the 4-methoxyphenyl enones shows antimicrobial potential against their microbes.

A series of Imidazo-propenones were evaluated for their cytotoxic effects against human cancer cell lines A549 (lung adenocarcinoma epithelial cell line). Quantitative Structure-Activity Relationship (QSAR) has been investigated in a series of 23 imidazothiazole-prop-2-en-1-one derivatives to correlate the activities and structures, using DFT and 2D-QSAR. The compounds were obtained by molecular descriptors encoding a small part of the whole chemical information of the molecule. The principal component analysis PCA; linear (Multiple linear regressions (MLR)); nonlinear (artificial neural network); and the regression partial least squares (PLS) mo dels were used to relate the structural features to their reported activities. The ANN model was tested by leave-one-out-cross-validation reliably and unbiasedly estimates prediction errors, also to assess the significance of the model and to predict biological activities of other novel compounds. In this work, the results obtained indicate...

An effective synthetic process for the preparation of 3-Benzyl-6-methyl-7-oxa-3-aza-bicyclo[4.1.0]heptanes 7 and 3-Benzyl-6-methyl-3,7-diazabicyclo[4.1.0]heptane-7-carboxylic acid tert-butyl ester 9 has been developed from simple synthetic transformations , starting with extraordinarily simple materials (4-picoline and benzyl chloride) in five steps through reduction and epoxidation followed by ring opening, providing a new and convenient access to the key intermediates of Tofacitibin (CP-690,550).The process developed is highly efficient and can be applied for large scale synthesis also. 

For the estimation of Rabeprazole in bulk and tablet dosage form two simple and sensitive methods have been developed. In Method 1 folin– ciocalteu reagent and sodium hydroxide is used. Folin–Ciocalteu reagent reduced in the presence of sodium hydroxide by the Rabeprazole andblue coloured chromogen is formed, exhibiting absorption maxima at 640 nm and at a concentration range of 1–8 μg/ml linearity was obtainedwith correlation coefficient (r2) 0.9983 . In method 2 rabeprazole reduced ferric nitrate. The reduced ferric ions reacts with 2,2, bipyridine, exhibiting absorption maximum at 522 nm and at concentration range of 2-16 µg/ml linearity was obtained with correlation coefficient (r2 ) 0.9994. According to ICH guidelines these two methods are validated and the methods were suitable for estimation of Rabeprazole in bulk and pharmaceutical dosage form. 

A simple, fast and effective method for Assay of Metformin along with its usual combination drugs viz: Glipizide, Gliclazide, Glibenclamide and Glimepiride has been developed for simultaneous determination for Assay of each drug from separate combination tablet of each dosage form. The developed method was validated and proved to be precise and robust. Area response were found to be linear in the concentration range of 50 ppm to 150 ppm for Metformin, 0.5 ppm to 1.5 ppm for Glipizide, 8 ppm to 24 ppm for Gliclazide, 0.5 ppm to 1.5 ppm for Glibenclamide and 0.2 ppm to 0.6 ppm for Glimepiride. The correlation coefficient was found to be 0.9991 for Metformin, 0.9994 for Glipizide, 0.9997 for Gliclazide, 0.9998 for Glibenclamide and 0.9994 for Glimepiride.

Albendazole is a low water soluble benzimidazole carbonate drug, extensively used against instestinal parasites due to its broad spectrum activity, good tolerance and low cost. The drug has a disadvantage of poor bioavailability due to very low solubility in water. The main objectiveof the study was to increase the solubility and dissolution rate by complexing with cyclodextrins by kneading method and to compare thesolubility between hydroxypropyl beta cyclodextrin and beta cyclodextrin . Solid state characterization was done by Fourier Transform Infrared (FTIR) and thermo gravimetric analysis. Increased solubility was obtained when more substituted cyclodextrins were used instead of nonsubstituted cyclodextrins. High oral dose of albendazole is required for treating systemic helminthiasis which can lead to liver impairment, so the main aim of the study was to analyze liver enzymes using albino wistar rats. For enzyme determination, blood samples were collected from each rat after 48 ...

A simple, fast and effective method for Assay of Metformin along with its usual combination drugs viz: Glipizide, Gliclazide, Glibenclamide and Glimepiride has been developed for simultaneous determination for Assay of each drug from separate combination tablet of each dosage form. The developed method was validated and proved to be precise and robust. Area response were found to be linear in the concentration range of 50 ppm to 150 ppm for Metformin, 0.5 ppm to 1.5 ppm for Glipizide, 8 ppm to 24 ppm for Gliclazide, 0.5 ppm to 1.5 ppm for Glibenclamide and 0.2 ppm to 0.6 ppm for Glimepiride. The correlation coefficient was found to be 0.9991 for Metformin, 0.9994 for Glipizide, 0.9997 for Gliclazide, 0.9998 for Glibenclamide and 0.9994 for Glimepiride. 

For the purpose of finding additional metal based anticancer medications with lower toxicity and higher affectivity, Pd(byp)Cl2 complex, where byp is 2,2-bipyridine, was characterized and synthesized. The formed stable and Stoichiometric constants between different bimolecular targets(ligands) that have diverse functional groups and accessible in vivo such as, amino acids, amides, DNA unit constituents and [Pd(byp)(H2O)2] 2+ were examined at constant ionic strength of 0.1 mol.dm-3 and at 25ºC. The diverse classes' concentrations were evaluated utilizing distribution diagrams. Moreover, the [Pd(byp)(H2O)2] 2+ complexes with different chosen ligands were formed and characterized.

In this work, the electrochemical reduction of some Schiff’s bases contains substituted coumarin moiety and the effects of the substituents have been studied by polarographic technique. Based on the results obtained and previous literature, a tentative mechanism has been proposed. Thesystem investigated in this study was a series of substituted (17Z)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N'-benzylideneacetohydrazides. The system possesses two electrophores; (1) Hydrazone group and (2) Carbonyl group. Thus, the electrochemical reduction of the system, studied with DC polarography, might provide valuable insight into the processes taking place on the surface of the electrode and can be of importance in fundamental electrochemical research.

An electrochemical sensor for the detection of insulin was fabricated, using the electrochemically deposited CCLP- Au NPs modified electrode. The morphology and structure of the CCLP- Au NPs are characterized by Scanning Electron Microscopy (SEM), X-ray Diffraction (XRD), UVVisible spectroscopy (UV-Vis) and Transmission Electron Microscopy (TEM) studies. The building of the immunosensor was evaluated in each and every step by Cyclic Voltammetry (CV) and Impedance spectroscopy (EIS). The electrochemical detection was based on the anti-insulinHRP (Horseradish Peroxidase) bundled with Au NPs which binds to the immune complex and the response was observed using Hydro Quinone (HQ) and Hydrogen peroxide (H2O2 ) in phosphate buffer electrolyte. From the results, the sensitivity range is from 50 to 556 pM/l and LOD is calculated as 2.14 pM/l (3σ/s). The developed immunoassay has the ability to insulin in human blood serum samples of healthy individuals.  

A number of pre-designed C-7-substituted-2-morpholino-N-(pyridin-2-ylmethyl)quinazolin-4-amine were synthesized for the first time using Palladium catalyzed suzuki reactions in microwave with a ligand X-PHOS. A key intermediate 7-chloro-2-morpholino-N-(pyridin-2-ylmethyl)quinazolin-4-amine (7) was synthesized and treated with 20 different boronic acids to give 20 derivatives in good to excellent yields. All these compounds were tested for their antibacterial properties against four strains of bacterial microorganisms including two gram-positive and two gram-negative species. Out of twenty compounds, five compounds, compound 8, 16, 23, 24, 25 showed better activity against gram negative as well as gram positive strains. 

The approach of green synthesis of silver nanoparticles was focused in the present work using leaf extract of two medicinal plants, Averrhoa bilimbi L. and Syzygium cumini L. in different intensities of sunlight. The method is light sensitive, simple, eco-friendly and quick for the synthesis of AgNPs from leaf extracts. These plants extract mediated SNP’s were comparatively characterized and evaluated for their antioxidant properties independently. The synthesized AgNPs were characterized by UV-spectroscopy, Nanoparticle Tracking Analysis (NTA),X-ray Diffraction (XRD), Transmission Electron Microscopy (TEM) and Fourier Transformed Infrared spectrum (FTIR) analysis. The UVspectra showed maximum absorbance at 430 nm, NTA analysis shows 20 nm average sizes of AgNPs synthesized in A. bilimbi and 50 nm size in S. cumini leaf extract respectively. XRD analysis showed four Bragg’s reflection planes of the metallic silver in the 2θ range of 30º-80º and indexed as (111), (200), (220) and (311...

Naphthyridine derivatives have received significant attention due to their exceptionally broad spectrum of biological activity. Nalidixic acid, forexample, possesses strong antibacterial activity and is used mainly for the treatment of urinary tract infections with gram-negative pathogens [1]. Gemifloxacin possess both antimicrobial properties [2] whilst 1,8-naphthyridine derivatives have promising medicinal properties such as antiHIV [3], anticancer [4], anti-inflammatory [5], antimalarial [6], antibacterial [7], antiprotozoals [8], antimycobacterial [9] and antiplatelet [10]. Moreover, it was recently found that 1,8-naphthyridine derivative vosaroxin (formerly SNS-595, AG-7352, AT-3639, or Voreloxin) was found to have potential anticancer activity; it is currently subjected to clinical development. This drug is reported to exert its action via topoisomerase II inhibition [11]. Topoisomerase II is one of the well-known targets for antitumor agents like doxorubicin, etoposide, ellipti...

Water is one of the major components of life for living being on earth. On the earth, it is abundant and most unusual natural component. Hand pumps, wells, ponds and rivers are the common resources for villages of Dhar district, a tribal belt area. Among them water quality of hand pump is degrading continuously with faster rate and therefore it is essential to monitor water quality time to time and treatment, if needed before use of drinking purpose. The present manuscript deals with fluoride concentration at Umarban and Tirla blocks of Dhar district ofMadhya Pradesh.  Various drinking water sources of Umarban and Tirla blocks of Dhar district were specified and selected for sampling and their fluoride concentration were analyzed. The fluoride concentration in Khandan Bujurg (S-3), Ghanora (S-26) and Kuwa (S-21) water sources, is much higher than Badlipura (S-8), Dhanora (S-27) and Banzari (S-29) etc. These water sources having high fluoride concentration are marked as red. It is ...

Since their discovery, essential oils are known as a hugely valuable resource to treat a variety of infections due to their multiple biological functions, especially their antimicrobial, and antioxidant activities. Unfortunately, these volatile compounds have also certain limits such as the processes for extracting of these oils, the purification of their bioactive molecules and their minimal amount. For that reason several scientistshave been oriented their research towards synthetic molecules as a new tool to overcome the progression of many chronic diseases (cancer, fibrosis, cirrhosis, arthritis). The prime focus of this work was the synthesis and characterization of four α-aminophosphonate derivatives 4(a-d). Then we evaluated their antioxidant activity against oxidative and nitrosative stress. The in vivo experiments are conducted using Tetrahymena protozoan treated with IC50 of hydrogen peroxide (H2O2 ) or sodium nitroprusside (SNP); finally we checked their antioxidant behav...

A new stability-indicating chromatographic ultra-performance liquid chromatography (UPLC) method has been developed and validated for determination of Perindopril Arginine (PER) and Amlodipine Besylate (AML) in their dosage form and in the presence of their degradation products. The method was based on ultra-performance liquid chromatography, by which the components were separated on a Acquity UPLC BEH C18, 1.7 µm, 2.1 × 50 mm. part no.186002350 column, using a mobile phase consisting of phosphate buffer pH 2 and acetonitrile (75:25) with ultraviolet detection at 210 nm. Different parameters that affect this new method were optimized to achieve maximum separation for those components. Both drugs were subjected to forceddegradation studies under hydrolysis (acidic, alkaline and oxidative stress). The proposed method is considered as stability indicating because of the resolution of the aforementioned drugs from their degradation products. Moreover, the degradation products for both dr...

The concentration of fluoride in common dentifrices can be found using various methos. An ion selective electrode can be used to continuously measure the concentration of fluoride in various toothpaste suspensions. Using an ion selective electrode, compared to high performance liquid chromatography and ion chromatography, requires a short amount of time required for sample preparation and gathering experimental data. The quick monitoring of fluoride in toothpaste using an ion selective electrode.Thiscan ensure that the specified fluoride content is accurate and effective against fighting cavities in teeth. If the toothpaste samples contain large amounts of fluoride, they may cause fluorosis; however, smaller amounts may not properly protect teeth. Creating suspensions of toothpaste can be used to ensure advertised fluoride contents match actual fluoride contents, while mirroring the oral environments toothpastes are used in. In this study, fluoride ion content has been measured in se...

A novel rubber-nanocomposite has been synthesized through the emulsion polymerization of styrene-butadiene rubber and nano antimony oxide using accelerators and antioxidant. Sulphur was used as vulcanizing agent. The synthesized SBR-nano antimony oxide was characterized by elemental analysis, FTIR, scanning electron microscopy, transmission electron microscopy and mechanical testing. On basis of the FTIR, the structure of the SBR-nano antimony oxide was proposed. The physico-chemical parameters have been evaluated for the SBR-nano antimonyoxide. The aggregation nature of the synthesized rubber-nano composite was established by scanning electron microscopy (SEM). The effects of nano particles in polymer matrices have been evaluated for the SBR-nano antimony from TEM analysis. Mechanical behavior of the composites are found to improve consistently as nano- antimony oxide content in the composites increases owing to increased rubber- filler interaction. Tensile strength studies are fou...

The trituration of olives in Morocco is ensured by a different system of extraction. Traditional units triturate approximately 30% of the national production, whereas the 70% are treated by semi-modern units using super-presses and industrial units employing the continuous system twophase and three-phase. The physicochemical characterization of the pomace obtained from different extraction systems has revealed a high moisture content, a slightly acid pH (5.9 - 6.04) and a high content of organic matter (74.69% to 92.03%). The pomace studied is rich in nutrients important for the growth and development of plants. In effect, it is rich in potassium, carbon, and oligo-elements. However, these properties are compatible with the requirements of the agriculture of several plants, reason for which this pomace can be considered as a soil amendment especially those that are poor in organic matter, namely the Mediterranean soils.  

In the present work our goal was to explore the prodrug approach study especially for colon targeting antibacterial agents. We choose the sulfonamides as an antibacterial agent for colon targeting treatments. For this purpose sulfonamides were coupled to carvacrol through azo compound formation. The newly synthesized azo compounds were characterized by spectral techniques such as Infrared (IR), Proton Nuclear Magnetic Resonance (1H-NMR) and Carbon-13 Nuclear Magnetic Resonance (13C-NMR). The drug released study of the parent compound was done by in vitro enzyme degradation by using azoreductase enzyme which was secreted by pseudomonas aeruginosa bacterium. Carvacrol and its derivatives were known show remarkable biological activity such as antimicrobial, antitumor, antimutagenic, antigenotoxic, analgesic, antispasmodic, anti-inflammatory, angiogenic, antiparasitic, antiplatelet,