Derpharmachemica

Terminalia chebula, popularly known as Harad, black- or chebulic myrobalan contains hydrolysable tannins. This dominantly contains many phytochemicals viz., casuarinin, chebulanin, chebulagic acid, chebulinic acid corilagin, ellagic acid, gallic acid, neochebulinic acid, punicalagin, 1,2,3,4,6-penta-O-galloyl-β-D-glucose,1,6-di-o-galloyl-D-glucose,3,4,6-tri-o-glloyl-D-glucose, terchebulin. There are many medicinal investigations recording viz., antiulcer, antioxidant, anticarcinogenic, antimutagenic, radio protective, hepatoprotective, cardioprotective, cytoprotective, antidiabetic, renoprotective, antibacterial, antifungal, antiviral, antiprotozoal, anti-inflammatory, antiarthritic, antispasmodic, wound healing and anticonceptive, molluscidal, anthelmintic, anaphylactic, hypolipidemic, hypocholesterolemic. Also having chemopreventive potential and adaptogenic activities. This has purgative property, immunomodulatory, analgesic, antiallergic, neuroprotective, acetylcholine inhibition ...

A novel method for the estimation of Budesonide in human plasma by using LC-MS-MS and the analyte is budesonide and internal standard is levenorgestreol were extracted with the tertbutyl methyl ether: n-hexane (70:30, v/v) from human plasma. The chromatographic severance was attained of the peak using Agilent Zorbax Eclipse XDB-C8 , (100 mm × 4.6 mm, 3.5 µm) column with a run time is 2.5 min. Budesonide andlevenorgestreol were recorded at the total ion current of their relevant multiple reaction monitoring. The LC-MS-MS system composed an Agilent 1100 infinity combined with an AB Sciex Qtrap® 4000 thermo Finnigan TSQ quantum discovery triple quadruple mass spectrometer. All of the parameters must be validated like selectivity, accuracy, precision, linearity, lower limit of quantification, matrix effect, recovery reached the acceptance criteria under the following of ICH guidelines. Budesonide have checked the various stability studies like short term stability at 25°C, long term stab...

The purpose of the present study is to evaluate the anti-inflammatory activity of the fresh extract obtained from the fruits Bougainvillea glabraLinn. in rats. The fresh juice extracted from the flowers of B. glabra Linn. were evaluated for the anti-inflammatory activity by using the carrageenan induced model in rats at a doses of 100 mg/kg and 200 mg/kg respectively. Biochemical parameters like paw oedema were studied. The B. glabra contains the phytochemical constituents like steroids. The fresh extract of B. glabra flowers showed the significant reduction in the paw volume at the doses of 100 mg/kg and 200 mg/kg. The results suggest that the flower extract of the Bougainvillea possess anti-inflammatory effect. The observed effect may be due to the presence of bioactive constituents.

The present investigation describes the adsorption of Methyl Violet (MV) dye onto Creeson (Lepidium sativum) (LS) seeds known as Garden cress from its aqueous solution, has been known centuries ago in eastern regions then spread worldwide. The using of creeson seeds asadsorbent for the removal MV dye was investigated in aqueous solution. Effect of experimental coefficient like connection time, primary concentration of adsorbate (MV) and amount of adsorbent seeds (LS) dose and temperature were evaluated to obtain the optimum condition for adsorption of MV onto Cresson seeds using batch adsorption. The adsorption information were mathematically analyzed using isotherms of adsorption like Langmuir, Freundlich and Dubinin-Radushkevich isotherms to study adsorption mechanism of MV dye onto creeson seed. The isotherms of adsorption were advanced and equilibrium data adjusted well to Freundlich isotherm model. The studies of kinetic indicated that the process of adsorption followed the mode...

Topoisomerases are class of enzymes that alter the super coiling of double-stranded DNA. (In super coiling the DNA molecule coils up like a telephone cord, which shortens the molecule.) The Topoisomerases act by transiently cutting one or both strands of the DNA. Topoisomerases are enzymes that regulate the over winding or under winding of DNA. The winding problem of DNA arises due to the intertwined nature of itsdouble-helical structure. During DNA replication and transcription, DNA becomes over wound ahead of a replication fork. If left unabated, this tension would eventually stop the ability of the enzymes involved in these processes to continue down the DNA strand. Topoisomerase inhibitors are agents designed to interfere with the action of topoisomerase enzymes (topoisomerase I and II), which are enzymes that control the changes in DNA structure by catalyzing the breaking and rejoining of the phosphodiester backbone of DNA strands during the normal cell cycle. The present review ...

We have synthesized novel 2-(4-(3a,4,5,6,7,7a-hexahydro-4,7-methanobenzo[d]isooxazol-3-yl)phenyl) imino)-3-methylthiazolidin-4-one and its benzilidine derivatives in good yields, by clubbing substituted Isooxazoline and 4-Iminothiazolidinone. All the synthesized compounds were characterized using IR and NMR spectroscopy. The results of the characterization are in agreement with the structures of compounds and testedfor its antibacterial and antifungal activity against various strains like Staphylococcus aureus (NCLM 2602), Bacillus subtilis (NCLM 2458), Escherichia coli (NCLM 2809), Aspergillus niger (NCLM 617), Rhizopus ostoyae NCLM 1299) by using antibacterial susceptibility test. All the newly synthesized compounds possess moderate to good antibacterial activity.

In the present synthesis work, we were synthesized viable bio active nitrogen and oxygen atom containing heterocyclic compounds like pyrazole, pyrazolone, coumarin, azo coumarin, and naphthyl coumarin. A metal catalyst free reaction to afford the targeted compounds (1-7) in goodyields. All three types of coumarins were synthesized in one step ecofriendly approach under solvent free condition. The beauty of this work easily available primary material, gentle conditions, smooth operation and economical cost. The synthesized compound structures were confirmed by advance spectroscopic techniques and elemental analysis. Besides, compounds also evaluated for their in vitro antimicrobial activity

Phenyl imidazole propionate derivative which shows wide range of biological activities was synthesized. The yield of imidazole ring formation i.e. conversion of 1-isopropyl 3-(2-oxo-2-phenylethyl)2-(4-methoxybenzyl)malonate (1) to tert-butyl 3-(4-methoxyphenyl)-2-(4-phenyl-1Himidazole-2-yl)propanoate (2) was improved from 35% to 87%. Statistical model based screening and optimization DOE study were carried outto derive the most favorable design space and optimal operating condition for the process parameters. The model of optimization study was created using central composite design. Model-validation was performed which showed excellent reproducibility with high degree of precession. Use of ammonium chloride as a catalyst to improve the yield of imidazole ring formation reaction was also explored for the first time

Allergic asthma is a complicated disorder where multiple stimuli activate various signalling pathways resulting in the synthesis of a wide array of inflammatory proteins. Among the diverse transcription factors in the human genome, Nucleus Factor Kappa B (NFκB) and p38 Mitogen Activated Protein (MAP) kinases play a crucial role in the pathophysiology of allergic asthma. Salicylic acid derivatives, 5-Amino Salicylic Acid(5-ASA) and Sodium Salicylate (SS) have been evidenced to inhibit NFκB in vitro model. 5-ASA has demonstrated significant antiasthmatic activity in preclinical murine models. In the present study, 5-ASA and SS were screened in silico against a definite set of proteins, namely Inhibitor of Kappa Beta (IκB), p38 α, β, γ and δ using Glide and Prime modules of Schrodinger suite. The two drug candidates were attributed to the MTT assay in RAW 264.7 mouse monocyte macrophage cells for their in vitro cytotoxicity. From the hits obtained in silico, IκB and p38γ were further e...

A reversed phase high performance liquid chromatography was developed for estimation and determination of two actives pharmaceutical ingredient Udenafil (Zydena) and Dapoxetine (Priligy). In presence of pregabalin as internal standard. The chromatographic conditions wereapplied according to ICH-guidelines using Thermo Hypersil BDS–C18 (250 mm × 4.6 mm, 5.0 µ) the mobile phase containing acetonitrile: 0.2% triethyl amine in pure water (H2O) the adjusted pH was 4.4 using ortho- phosphoric acid (75: 25) with flow rate amount approximately 1 ml/min using UV detection at 246 nm. Limit of detection was established to be 0.015 μg/ml and Limit of Quantification (LOQ) was found to be 0.025 μg/ml for udenafil and the Limit of Detection (LOD) of dapoxetine HCl 0.020 μg/ml. according to ICH-guidelines and statistical treatment of date the date for this method was linear with correlation coefficient R2 > 0.99 which prove that the method is convenient and applicable for the investigation and st...

A series of novel 1,3,5-triazine derivatives bearing various aryl amine, 2-amino pyrazine and 4-hydroxy coumarin moieties as substituents have been synthesized by an easy and conventional method using sequential nucleophilic substitution of chlorine atoms of cyanuric chloride. Thereaction of cyanuric chloride with 4-hydroxy coumarin in acetone using alkaline medium at 0-5°C was afforded compound 3 in good yield. Followed by reaction 3 with 2-amino pyrazine and then various aromatic amines have afforded target compounds 6a-n in good yields. All the newly synthesized compounds were characterized by using spectroscopic analysis and then examined for their ability to inhibit the two Grampositive bacteria (Bacillus subtilis and Staphylococcus aureus) Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and one fungal species (Aspergillus niger) for biological interest.

The outer rinds or peels of many fruits are not eaten and are thrown as a waste. Similarly in food industry, processing of fruits results in the formation of agro waste in high amounts and is common in the form of peels. This waste has to be managed efficiently as they pose seriousproblems to environment. Till now agro waste is used as livestock feed or as fertilizer but recently strategies have been developed to explore the bioactive components from the peels as well as their therapeutic benefits. Many scientific investigations reported the isolation of constituents with promising antioxidant, antimicrobial, antiproliferative activities from the peels of various fruits.

Complex anodic alumina films were preapered by the reanodization of porous anodic oxide films on aluminium alloy (AA) 5052. The AA 5052 samples were anodized first in H2SO4 for 30 min at 15 V. The reanodization was performed in 0.1 M ammonium pentaborate solution at 15 V for 5 and 10 min. Electrochemical impedance spectroscopy was employed to characterize these complex films. Polarization studies show that thecorrosion rate decreases significantly by reanodization and it is further decreases with an increase in reanodization time. Reanodization is found a good method to increase corrosion resistance properties of porous anodic oxide film. Morphologically, no significant difference was observed between simple and complex film as shown in Field Emission Scanning Electron Microscope (FESEM) images. The electrochemical impedance data was fitted with equivalent circuit containing a Constant Phase Element (CPE) and fitted parameters were calculated.

In the present study, a series of novel 3-chloro-1-(5-((2-oxo-2H-chromen-4-yl)thio)-4-phenyl thiazol-2-yl)-4-substituted phenyl azetidin-2-ones (7a-j) have been efficiently synthesized in five steps by the use of acetophenone, thiourea, 4-mercapto coumarin and chloro-acetyl-chloride. Thestructures of all the newly synthesized analogues were characterized by 1H-NMR, 13C-NMR spectroscopy and mass analysis. All the finalsynthesized analogues were examined for their preliminary in vitro antibacterial activity against Gram-positive (Staphylococcus aureus andStreptococcus pyogenes) Gram-negative (Escherichia coli and Pseudomonas aeruginosa) bacteria and antifungal activity against (Candida albicans, Aspergillus niger and Aspergillus clavatus) strains by using broth dilution technique. The results of antimicrobial study revealed that some of the newly synthesized compounds exhibits potent activity against the present specific microbial strains.

Many plants are important to cure various human ailments. India has a rich source of naturally occurring herbal plants which have huge as well as great pharmacological functions. A lot of medicinal plants are used in treating various disorders. Herbal medicines play a vital role inAyurvedic, Homeozpathic, oriental and Native American Indian medicine. Various pharmaceuticals companies conducting extensive research on plant materials which have high potential value. Cedrus deodara commonly called as cedar is precious plant belonging to family Pinaceae. C. deodara is a medicinal herb with a lot of beneficial as well as pharmacological activities which prove to be a boon in solving various health issues.  

The title compound 5-[3-(4-Nitrophenyl)-4,5-dihydro-1,2-oxazol-5-yl]Methyl-5H-dibenzo-[b,f]azepine, is synthesized and characterized using single crystal X-ray diffraction method. The azepine ring adopts boat confirmation and the fused benzene rings to the azepine ring makes adihedral angle of 53.39 (7)0. In the crystal structure, molecules are stabilized with the C-H ...π, N-O ...π and π...π short contacts. The intermolecular contacts in the crystal structures are quantified using Hirshfeld surfaces analysis method. The results suggests that the intermolecular H...H contacts contributes more to the crystal packing when compared to other contacts and the electrostatic potential surfaces are visualized.

The city of Salé produces about 24 millions m3 /year of wastewater. The majority of this water is discharged directly into the Atlantic coast and Bouregreg estuary without any treatment. To preserve the quality of the receiving waters. treating wastewater and reusing it in agricultureproves very interesting. The objective of this study is thus to investigate the treatment and recycling of wastewater in agriculture. We are particularly interested in studying the growth of the stem and the average number of leaves in order to prove the positive effects of reusing treated wastewater in agriculture as compared to untreated wastewater. To achieve this objective. we have investigated the irrigation of the broad bean by three types of water: Untreated wastewater (UW). Well water (WW) and biologically treated wastewater (TW).

Series of new heterocyclic compounds, Theinopyridines, Pyrazolopyridines and pyrazolopyrimidines derivatives were obtained by the reaction of sodium salt of 1-(4,5-diphenyl-1H-pyrrol-3-yl)ethanone with aminopyrazole derivatives, cyanothioacetaamide and cyanoacidhydrazide. Theobtained compounds were confirmed by spectroscopic analysis such as Infrared Radiation (IR) and Proton Nuclear Magnetic Resonance (1HNMR) and mass spectra. The newly synthesized compounds screened for antimicrobial activity against Gram-positive, Gram-negative bacteria and fungi. Pyrazolopyridines and Pyrazolopyrimidines showed anti-microbial, anti-bacterial and anti-fungal activities.

UV Spectrophotometric methodhas beendeveloped for estimation of lamivudine in bulk and tablet dosage form by using water as solvent. Method developed is Area Under Curve (AUC) method. For analysis of lamivudine by AUC method the wavelength range selected was 265nm to 275 nm because the linearity was obtained within this area with good reproducibility of results . Lamivudine shows absorbance maxima (λmax) at 271 nm scanned in UV range of 400 nm to 200 nm. Lamivudine obeys Beer’s law in the concentration range of 10-60 µg/ml.

The study is carried out to test the catalytic efficiency of Cu-ZSM-5 zeolite catalyst on the reaction of Aza Michael under solvent-free conditions, at room temperature this reaction is most exploited in organic chemistry, b-amino -esters, ketones, nitriles are useful for the preparation of several natural bioactive products, antibiotics, and chiral auxiliaries, through the use of the porous material catalyst (zeolite Cu-ZSM-5), and the reaction of Aza Michael addition a series of amines on α, β-unsaturated methyl acrylate, we have synthesized new cc or c-heteroatomproducts, these compounds is an attractive area of researchers in synthetic organic chemistry, and we have developed new synthesismethodologies for the preparation of these products. The reaction was carried out with favorable conditions: ambient temperature, and without solvent, that the products, which are synthesized, gave us a high yield, and excellent chemo selectivity.