251 research outputs found
Synthesis of Pharmacologically Relevant Arenes by [3+3] Cyclizations And Phytochemical Investigation of pulicaria undulata
Spirocyclische Cyclopropane wurden durch Umsetzung von Ketosulfon- und Cyanoaceton-Dianionen hergestellt und durch Behandlung mit Tetraalkylammoniumhalogeniden in funktionaliserte Arene überführt. Durch Cyclisierung des Dianions von Aceton und eines 3-Oxophosphonates konnten regioisomere Spirocyclopropane hergestellt und durch anschließende Umsetzung mit Tetraalkylammoniumhalogeniden in funktionaliserte Arene überführt werden. Es wurden Beiträge zur Synthese von Diarylethern, Biarylen und 1-Azaxanthonen geliefert. Weiterhin wurden Ergebnisse auf dem Gebiet der regioselektiven Synthese von Thiophenen durch Suzuki-Reaktionen von Tetrabromthiophen geliefert. Schließlich wurden neue Naturstoffe isoliert und charakterisiert.Spirocyclic cyclopropanes were made by reaction of ketosulfone and ketonitrile dianions. This was futher transformed to fuctionalized Arenes in the presence of tetraalkyl ammonium halides.By cyclization of the dianions from Acetone and 3-Oxophosphates it was possible to obtain regioisomeric spirocyclopropanes which were futher reacted with tetraalkyl ammoniun halides to obtain fuctionalized Arenes. Contributions were also made in the area of the Diarylether Biaryles and 1-Azaxanthones synthesis. Futher more contributions wre made in the area of regioselective synthesis of the Thiophenes by Suzuki reactions of tetrabromothiophene. Natural products were isolated and characterized
Analyzing the Impact of Globalization on Economic Growth
Globalization is a buzz word that catches significant importance as a reform agenda post 1980. The current study is an attempt to analyze the impact of globalization on economic growth of Pakistan. The sample period for this study ranges from 1980-2009. For empirical analysis of the study, Autoregressive Distributive Lag model is employed while for data analysis Augmented Dicky Fuller test is applied. It is found that all the variables are stationary at first difference. The empirical findings of the study suggest that economic globalization in long phase of time increase growth in case of Pakistan economy, social globalization has negative impacts on growth and political globalization is insignificant which mean that it will not increase or decrease the growth of Pakistan economy. While in short run economic globalization at lag 1 and social globalization decrease the pace of growth. It is suggested to the government that as overall globalization helps in increasing the growth of economy therefore government should formulate such a policy that helps the economy to be globalized. 
The anatomical, surgical and orthopedic importance of gastrocnemius
Gastrocnemius is one of the most important muscles of lower limb. It belongs to the superficial compartment of calf muscles. They belong to group of superficial flexors. Gastrocnemius, plantaris and soleus form the bulk of the calf. Gastrocnemius forms the belly of the calf. It arises by two distinct heads, connected to the condyles of the femur by strong, flat tendons. It has an immense anatomic, medical, orthopedic and physiological importance and is attributed in a variety of medical and surgical problems. A profound knowledge of this muscle is of great importance to any surgeon or orthopedicians or any clinician
Antioxidant, antimicrobial studies and characterisation of essential oil, fixed oil of Clematis graveolens by GC-MS
The GC-MS, antimicrobial and antioxidant activity of Clematis graveolens was assessed to explore its medicinal importance. Medicinal importance of its genus plants encourages us to undertake the comprehensive investigation of the essential oil and fixed oil of the leaves and stem. GC-MS analysis of essential and fixed oils showed the presence of many compounds in the leaves and stem parts of the plant like 2,2 dimethoxy butane (15.16%) flouroethane (45.14%) undecane (5.16), 1,2-benzenedicarboxylic acid (18.35), 3,8,12-tri-O-acetoxy-7-desoxyingol-7-one (12.74), propanoic acid, 2-(3-acetoxy-4,4,14-trimethylandrost-8-en-17-yl)- (9.14) and vitamine E acetate (4.38). The antimicrobial activity of the essential and fixed oil was resolute by disc diffusion and MIC (Minimum inhibitory concentration) assay and plant showed potent activity. Furthermore the antioxidant potential of essential and fixed oil was assessed by the DPPH, Reducing power and by percentage inhibition in linoleic acid system
Antibacterial, cytotoxic studies and characterization of some newly synthesized symmetrical N 3, N 3 ′ -bis(disubstituted)isophthalyl- bis(thioureas) and their Cu(II) and Ni(II) complexes
A series of some novel ,-bis(disubstituted)isophthalyl-bis(thioureas) compounds with general formula [C6H4 {CONHCSNHR}2], where R = 2-ClC6H4S (L1), 3,5-(Cl)2C6H3 (L2), 2,4-(Cl)2C6H3 (L3), 2,5-(Cl)2C6H3 (L4), and 2-NH2C6H4 (L5), and their Cu(II) and Ni(II) complexes (C1–C10) have been synthesized. These compounds (L1–L5) and their metal(II) complexes (C1–C10) have been characterized by elemental analysis, infrared spectroscopy, 1H NMR and 13C NMR spectroscopy, magnetic moments, and electronic spectral measurements. The ligands are coordinated to metal atom in a bidentate pattern producing a neutral complex of the type [ML]2. These compounds (L1–L5) and their metal(II) complexes (C1–C10) were also screened for their antibacterial and cytotoxic activities
Antioxidant Activity of Various Extracts and Organic Fractions of Ziziphus jujuba
Antioxidant effectiveness of indigenous medicinal plant Ziziphus jujuba shoots extracts and fractions with different polarity solvents (n–hexane, ethylacetate, methanol, chloroform) was assessed for total phenolics content (TPC), total flavonoid contents (TFC), DPPH radical scavenging activity and percentage inhibition of peroxidation in linoleic acid system. The shoots extracts and fractions contained appreciable levels of total phenolic contents 310-823 GAE (mg/100g Dry plant matter) and total flavonoid contents 210-650 CE (mg/100g of Dry plant matter). The Ziziphus jujuba extracts and various organic fractions also exhibited good DPPH 50% inhibition (IC50) ranges from 23.1µg/mL to 52.5 µg/ml and Inhibition of Peroxidation in Linoleic Acid 20.1 to 70.1%., respectively. Of the Ziziphus jujuba shoots extracts and fractions tested, 100% methanolic extract and 100% chloroform fraction exhibited the maximum antioxidant activity, the results of the present investigation demonstrated significant (p< 0.05) variations in the antioxidant activity. The results of the present comprehensive analysis demonstrated that Ziziphus jujuba shoots extracts and organic fractions are a viable source of natural antioxidants and might be exploited for functional foods and nutraceutical application
Controller Parameters Optimization for Multi-Terminal DC Power System Using Ant Colony Optimization
Voltage source converter based multi – terminal DC grids (VSC – MTDC) are widely used for integration of renewable resources. Control of these grids requires vector control method, which includes inner and outer current controllers, tuning of these controllers is very important. Conventionally used tuning methods consider approximated linear model to tune the proportional – integral (PI) parameters of voltage source converter (VSC) which fails to produce optimum disturbance rejection results. In this research an Ant Colony Optimization (ACO) technique is used to get the optimum parameters of inner and outer power control layers for multi – terminal DC system. ACO is applied simultaneously on inner and outer control layers and results are compared with classical tuning method. In this paper, a four terminal VSC – MTDC has been used under different sequence of events of disturbances e.g. load change on AC side, active power reference change for inverter and rectifier mode and disconnection of one terminal to evaluate the robustness of ACO algorithm with respect to classical method. The proposed tuning method gives superior results under different disturbance compared to conventional method.publishedVersio
Synthesis and molecular docking of new hydrazones derived from ethyl isonipecotate and their biological activities
Purpose: To investigate the antibacterial and α-glucosidase inhibitory activities of hydrazone derivatives (8a-h) of ethyl isonipecotate.Methods: The reaction of ethyl isonipecotate (2) with 3,5-dichloro-2-hydroxybenzenesulfonyl chloride (1) in an aqueous basic medium yielded ethyl 1-[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]piperidin-4- carboxylate (3). Compound 3 was subsequently converted to ethyl 1-[(3,5-dichloro-2-ethoxyphenyl) sulfonyl]piperidin-4-carboxylate (5) via O-alkylation. Compound 5 on reaction with hydrated hydrazine yielded 1-[(3,5-dichloro-2-ethoxyphenyl)sulfonyl]piperidin-4-carbohyrazide (6) in MeOH. Target compounds 8a-h were synthesized by stirring 6 with different aromatic aldehydes (7a-h) in MeOH. All the synthesized compounds were structurally elucidated by proton nuclear magnetic resonance (1H-NMR), electron impact mass spectrometry (EI-MS) and infrared (IR) spectroscopy. For antibacterial activity, solutions of the synthesized compounds were mixed with bacterial strains, and the change in absorbance before and after incubation was determined. For enzyme inhibitory activity, change in the absorbance of mixtures of synthesized compounds and enzyme before and after incubation with substrate was determined.Results: The target compounds were synthesized in appreciable yields and well characterized by spectral data analysis. Salmonella typhi was inhibited by 8e (MIC 8.00 ± 0.54 μM), Escherichia coli by 8f (8.21 ± 0.83 μM), Bacillus subtilis by 8c (8.56 ± 0.63 μM) and Staphylococcus aureus by 8c (8.86 ± 0.29 μM). Two compounds, 8e and 8d, were very effective inhibitors of α-glucosidase with IC50 values of 40.62 ± 0.07 and 48.64 ± 0.08 μM, respectively.Conclusion: Low IC50 values of the synthesized compounds against α-glucosidase demonstrates their potential in type-2 diabetes treatment. Furthermore, these compounds exhibit substantial antibacterial activity against the bacterial strains tested.Keywords: Antibacterial activity, α-Glucosidase inhibition, Ethyl isonipecotate, Hydrazo
Development and validation of a spectroscopic method for the simultaneous analysis of miconazole nitrate and hydrocortisone acetate in pharmaceutical dosage form
Purpose: To develop a new analytical method for the quantitative analysis of miconazole nitrate (MCN) and hydrocortisone (HCA) in pharmaceutical creams.Methods: The study was accomplished in three steps. In the first stage, a spectroscopic method was developed for the simultaneous analysis of miconazole (MCN) and hydrocortisone (HCA). For this purpose, serial dilutions of both drugs were prepared using ethanol: water (50:50) as the solvent system. All solutions were analyzed for absorbance spectrophotometrically at 205 and 249 nm for MCN and HCA, respectively. The method was validated for linearity, range, accuracy, precision and robustness. A commercial formulation was also assayed by the proposed method.Results: The absorbance data were linear over a concentration range of 1 to 12 μg/mL for MCN and 1 to 40 μg/mL for HCA, with correlation coefficient of 0.9995 and 0.9984, respectively. Limit of detection (LOD) and of quantification (LOQ) of MCN were 0.49 and 1.49 μg/mL, respectively, and for HCA, 1.50 and 4.57 μg/mL, respectively. The assay results for the commercial formulation were within the limits specified in British Pharmacopoeia.Conclusion: Simultaneous quantification of miconazole (MCN) and hydrocortisone (HCA) by UV spectroscopy provides a simple, reliable and robust method for the characterization of a mixture of the drugs in a dosage form.Keywords: Simultaneous analysis, Miconazole nitrate, Hdrocortisone acetate, UV-visible spectroscopy, Method validatio
Synthesis and consecutive reactions of a-azido ketones: a review
This review paper covers the major synthetic approaches attempted towards the synthesis of α-azido ketones, as well as the synthetic applications/consecutive reactions of α-azido ketones
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