Derpharmachemica

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 ...

The present invention describes the improved process for the preparation of dabigatran etexilate mesylate and impurities synthesis. TheSynthesis involves easily available commercial raw materials with Acylation from n-hexyl chloroformate makes to get desired DabigatranEtexilate from the methane sulfonic acid it is finally as a dabigatran etexilate mesylate salt with an effective yield. Catalyst free and pressure handled reactions are not performed. Dabigatran is an effective oral prodrug of the thrombin (Factor IIa) inhibitor it has been approved by FDA and is widely used to reduce the risk of stroke in patients with non-valvular atrial fibrillation.

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

Acinetobacter baumannii is a ubiquitous Gram-negative bacillus bacterium that is frequently found in the nosocomial infections. Regard to the rapid development of resistance against various antimicrobial agents due to the high ability of natural genetic transformation, A. baumannii is resistance to many of the antibiotics. Toxin-antitoxin system is one of the virulence agents in A. baumannii that can be involved in the emergenceof drug resistance. HicB as a toxin system is an ideal target for the design of new classes of antimicrobial agents against A. baumannii. The goals of this work was to model the complete tridimensional structure of the HicB protein using computational methods and to assess structural and functional of it. The consistency of modeled structure was confirmed by different servers to high accuracy for modeling and dynamics simulation. The molecular dynamic simulation and virtual screening results indicate that HicB is a stable protein from A. baumannii. These result...

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.