The term antioxidant is used for two groups of substances, industrial chemicals and natural chemicals found in body tissue and foods which are said to have vital health effects. The antioxidant activities of methyl and chlorine substituted 2-(2-alkyl/arylaminothiazol-5-oyl)-N-methylbenzimidazoles are studied using BHA as standard. The standard solution and the title compound were prepared with different concentration and a graph is plotted and from the graph the percentage reduction and IC50 value is calculated.
This work aims to identify and optimize leads for Imidazole derivatives as Pf dihydrofolatereductase and farnesyltransferase inhibitors. We designed 30 Imidazole derivatives and synthesized 18 best compounds on the basis of glide score. Glide score was obtained using GLIDE module (version 9.1, Schrodinger, LLC, New York, 2010). Molecular docking study of the designed ligands was performed to study the binding pattern of the structure with the enzyme. Total 18 compounds showed a very good binding pattern with the enzyme and were synthesized. The characterization of all the synthesized compounds were performed by TLC and various spectroscopic techniques. In vitro antimalarial evaluation of all the synthesized compounds (S1-S18) was performed. Biological activity mean IC50 (µg/ml) of all synthesized compounds (S1-S18) were determined. The activity of S15 compound is 0.023µg/ml which is comparable to chloroquine and the activity of S7 compound is 0.26 µg/ml which is comparable to quinine as antimalarial agent.
A rapid and precise reverse phase high performance liquid chromatographic method has been developed for the validated of Glecaprevir and Pibrentasvir, in its pure form as well as in tablet dosage form. Chromatography was carried out on Sunfire C18 (4.6×250mm) 5µ column using a mixture of Water and Acetonitrile (60:40% v/v) as the mobile phase at a flow rate of 0.9ml/min, the detection was carried out at 220nm. The retention time of the Glecaprevir and Pibrentasvir was 3.0, 3.8±0.02min respectively. The method produce linear responses in the concentration range of 25-125µg/ml of Glecaprevir and 10-50µg/ml of Pibrentasvir. The method quality for the determination of assay was below 2.0%RSD. The method is important in the quality control of bulk and pharmaceutical formulations.
M. Vineela*, Kavitha Waghray, S. Ramya Sri, B. Sri Latha.
A rapid and accurate reverse phase high performance liquid chromatography method has been developed for the validation of empagliflozin and linagliptin in pure form and in the form of tablets. Chromatography was performed on an Altima C18 column (4.6 x 150 mm, 5 μm) using water: ACN (15: 85% v / v) as the mobile phase at a flow rate of 1.0 ml / min. at 234nm. The retention time of empagliflozin and linagliptin was 2,088, 6,068 ± 0.02 min, respectively. The method produces linear responses in the concentration range of 5-25 μg / ml empagliflozin and 30-150 μg / ml linagliptin. The precision of the method for the determination of the test was lower than 2.0% RSD. The method is useful for the quality control of bulk and pharmaceutical formulations.
B. Sri Latha*, Kavitha Waghray, S. Ramya Sri, M. Vineela.
The present study was carried out on Naftopidil by employing solid dispersion technique. The λmax of phosphate buffer pH 6.8 of Naftopidil were found to be at 282 nm. The pure drug the optimised Solid dispersion formulations were subjected to FTIR studies. The results were showed that there's no interaction between the drug and excipients. The micrometric properties of blend of Naftopidil solid dispersion were characterized with respect to Angle of repose, bulk density, tapped density, Carr’s index and Hausner’s ratio. All the Values of batches indicating good flow properties. All the tablets of various batches complied with the official demand of weight variation as their weight variation passes the bounds. The hardness of the tablets ranged from 2.5±0.03 to 2.75±0.01 kg/cm2 and the friability values were less than 1% indicating that the tablets were compact and hard. The thickness of the tablets ranged between 3.01±0.32 to 3.06±0.54 mm. All the formulations satisfied the content of the drug as they contained 97.1 -101.4 % of Naftopidil and good uniformity in drug content was observed. Thus all the physical attributes of the ready tablets were found to be much among management limits. The dissolution profile of Naftopidil tablets were compared between solid dispersion tablets. The Naftopidil solid dispersion tablets showed better release in phosphate buffer pH 6.8, in that F8 showed good drug release i.e., 99.74 at 60 minutes. F8 formulation was taken as optimised formulation.
The present study is aimed to assessing the toxicity of the heavy metal chromium on the histology of labeo rohita fingerlings was studied. The fingerlings were exposed for 10,20 and 30 days in 10% sublethal concentration of 96 hrs Lc5o of chromium (3.5ppm). During this period fishes were fed with artificially prepared food (on the 10th, 20th, 30th day fishes) were taken out, sacrificed and the tissues of gill and liver were excised out. The Gill exposed to sub lethal concentration of chromium showed mild histological study during 10 days, of exposure. After 30 days fusion of gill lamellae, hypertrophy and degeneration of epithelium is prominent. Liver lesions consisted of vacuolation, degeneration of hepatocytes and degeneration of cell boundaries of hepatocytes. These result showed that the degree of distortion of the gill concentration of the metals was found to be dose and time dependent.
Capecitabine is an anticancer drug which is widely used in the treatment of breast cancer. However, its clinical application for cancer treatment has been greatly limited due to its low bioavailability. To tackle this problem, pluronic conjugate micelles, which are amphiphilic copolymers, were designed and evaluated in this study. These highly stable micelles with capecitabine in the core were formulated by slurry method using span 60, mixed span60/pluronic F127, mixed span60/pluronic P85 and cholesterol. The prepared Capecitabine niosomes were characterized for particle size, PDI, zeta potential. FTIR and DSC studies revealed that there was no interaction between the drug and Excipients. SEM studies showed nearly spherical shaped vesicles. F6 showed highest % drug content (99.51±0.36), % entrapment efficiency 85.03±0.54% and % of in-vitro release 98.82±0.47% was obtained at 24th hour. In-vitro kinetics release rate for the all formulations followed zero order mechanism. The Optimized F6 formulation was subjected to three months for stability studies at temperature 5°C ± 3°C showed that there is not much variation in the vesicles size, % drug retained and cumulative percentage of drug release.
A series of 5-(5-amino-1, 3, 4-oxadiazol-2-yl)-3, 4-dihydro-6-methyl-4-phenylpyrimidin-2(1H)-one derivatives have been synthesized, by changing various substituted benzaldehyde. Simple synthetic methods of 5-(5-amino-1, 3, 4-oxadiazol-2-yl)-3, 4-dihydro-6-methyl-4-phenylpyrimidin-2(1H)-one (3a-e) are described. Compound 1 is converted to hydrazine carbothiamide2 by reacting compound 1 with thiosemicarbazide in catalytic amount of acetone is irradiated with help of domestic microwave oven (200W) for 2 minutes. Compound 2is an intermediate for the final compounds. The compound 2 is converted to corresponding oxadiazole3 by treatment with NaOH follow by KI. Structural elucidation is accomplished by IR, 1H and 13CNMR, Elemental analysis and GC-Mass spectral data of the synthesized compounds. Few of these Pyrimidine derivatives have been evaluated for their possible antibacterial activity. Most of the tested compounds show significant antibacterial activity.
The graphene, graphene-based as well as graphene/MoS2 hybrid composite are promising for applications in energy storage devices due to the intriguing properties, such as, highly tunable surface area, outstanding electrical conductivity, good chemical stability and excellent mechanical behaviour. While graphene itself is chemically inert and a gapless semimetal, its isostructural analog, molydenumdisulfide (MoS2) is chemically versatile with band gaps, thereby finding significant use in a myriad of applications. Although this 2D nanomaterial individually possesses tremendous authority for various applications, the combination of these materials in the recent past has created a new paradigm in emerging applications. Here, I try to attempt a comparative study between grapne/graphene-based vs graphene/MoS2 hybrid materials in the applications as energy storage devices.
Cancerous growth is one of the major causes of worldwide human mortality. An outsized variety of antineoplastic medication are existed within the market and most of the compounds are below clinical trials. Different studies discovered that these antineoplastic medication have shown the various kinds of effects, thus researchers round the world are engaged within the coming up with of additional economical and novel antineoplastic medication. In gift years, Quinazoline and its derivatives are thought-about as a completely unique category of growth chemotherapeutical agents that shows of activity against totally different tumours. Quinazoline are a large class of active chemical compounds exhibiting a broad spectrum of biological activities in animals as well as in humans and it is one in all the foremost fascinating novel bioactive compounds amongst all the heterocyclic compounds. Various of research and review papers have shown the development of Novel Quinazoline derivatives for cancer therapy. This review was focussed on the Quinazoline derivatives with antineoplastic activity.