SYNTHESIS OF SOME NOVEL PYRAZOLE DERIVATIVES AND EVALUATION OF THEIR PURIFICATION OF CHROMATOGRAPHY IN THIN-LAYER CHROMATOGRAPHY

Objective: The main objective of the study is to synthesis some novel pyrimidine scaffold which has wide range of properties of biological activities.Methods: Synthesis of different pyrazole derivatives compounds identification and characterization (M.P, solubility, Rf values, and spectral studies). The present work was characterized by infrared, nuclear magnetic resonance, and mass spectral analysis pharmacological evaluation.Results: Identification and characterization (M.P, solubility, Rf values and spectral studies) are carried out

A COMPENDIOUS REVIEW ON THE METABOLIC SYNDROME; ITS IMPACT ON THE QUALITY OF LIFE

Background: Metabolic syndrome (MetS), a comprehensive condition is universally described as a group of several causative factors or abnormalities directly linked with insulin resistance that obviously augment the threat mainly for coronary heart disease, diabetes mellitus Type 2, some types of cancers and sleep disturbances, etc. MetS is a contemporary condition that covers a wide-ranging display of disorders with definite metabolic anomalies demonstrating at different times. Consequently, the threat of MetS remains epidemic. This review will potentially study significant factors such as central adiposity, insulin resistance, hypertension, and dyslipidemia; increased inflammation, environmental factors, and genetic predisposition are involved in MetS development. Purpose: This review provides the available facts to validate the relationship between MetS and quality of life. Methods: A thorough exploration in many search engines such as PubMed, Medline, Science direct, EMBASE, and Google scholar was carried out to recognize qualified studies. Results: Almost all studies suggested that MetS is significantly associated with impair quality of life. Lifestyle intervention holds the early preference and such non-pharmacological therapy combines specific suggestion on diet and physical activity with behavioral strategies. For the individuals, where contributing factors are not sufficiently condensed with lifestyle changes, pharmacological treatment should be considered. Conclusion: Therefore, the current study reviews the outline of literature interrelated with the MetS's characterization, epidemiological existence, pathological process, and management advance for all the risk factors encompassing metabolic disorder

MOLECULAR DOCKING STUDIES OF ISOLATED FLAVONOIDS COMPOUNDS FROM AMARANTHUS TRISTIS LINN. AS ALPHA-AMYLASE AND ALPHA-GLUCOSIDASE ACTIVATORS

Aim: Aim of this work on in silico approach to used to access the use of flavonids compounds of nutritionally enriched plant Amaranthus tristis Linn.Methods: Bioflavonoids of rutin isolated from A. tristis Linn. and active agents receptor such as alpha-amylase (1SMD) and alpha-glucosidase (3wy1) activators. Three-dimensional structure of receptors was obtained from protein data bank database and biocomponents such as isoflavones and flavonones of A. tristis were downloaded from database like USDA. Docking studies of insulin receptor with A. tristis biocomponents for isoflavones and flavonones were performed using AutoDock - 1.5.6 software.Results: Compounds from A. tristis Linn. showed better binding features with the alpha-amylase and alpha-glycosidase. Thus, these compounds can be effectively used as drugs for treating diabetes which is predicted on the basis of docking scores.Conclusion: The insights gained in this work can be further used in experimental studies for designing antidiabetic drugs with novel targets and mode of action

SYNTHESIS, CHARACTERIZATION, AND EVALUATION OF ANTIFUNGAL PROPERTIES OF SUBSTITUTED BENZIMIDAZOLE ANALOG

Objective: The aim of the present study is to synthesize novel benzimidazole derivatives as potent antifungal agents.Methods: 2-chloromethyl-1H-benzimidazole has been synthesized by refluxing o-phenylenediamine with chloroacetic acid in the presence of 5N HCL. Further, N-substituted benzimidazole derivatives containing various heteroamines and aromatic compounds were synthesized. These, finally, prepared derivatives were kept for in vitro antifungal property.Results: A novel series of antifungal agents, containing benzimidazole nucleus as a basic skeleton, has been synthesized.Conclusion: The synthesized novel benzimidazole derivatives exhibit moderate activity (VMSA 1, 2, 8), some compounds showed significant activity (VMSA 6, 9, and 10), and compound VMSA 4 and 5 exhibits maximum activity

COMPUTATIONAL STUDY OF BUTYL AND NAPHTHYL AMINE DERIVATIVE OF PERYLENE DIIMIDES TARGETTING TELOMERASE ENZYME FOR ANTICANCER ACTIVITY

Objective: Telomeres are protective caps present at the end of the chromosomes and it contains genetic information. From the literature survey, we selected perylene diimides which interact with the telomerase enzyme and possess anticancer activity. Telomestatin a macrocyclic chemical compound that inhibits telomerase activity as well it induces the formation of G-Quadruplex structures in the telomeric region. The main objective of the study was to find the binding affinity of butyl and naphthyl amine derivative of perylene ligands targeting telomerase enzyme for anticancer activity. Telomerase enzyme is responsible for maintaining the length of telomeres and keeping the chromosomes intact longer. Telomeres will become increasingly common with age. Perylene diimides and its derivatives show good biological activity and also in vitro studies possess efficient anticancer agent. The butyl and naphthyl amine derivatives are screened by computational techniques to study regarding binding energy and ligand interactions with respect to the targets.Methods: Butyl and naphthyl amine derivative of perylene diimides is drawn using Accelrys Draw. The structures are retrieved from the previous study. The structures are converted to pdb formats using Discovery Studio Visualizer 4.1. The study was to investigate the binding energy values of butyl and naphthyl amine derivatives of perylene diimides. Auto Dock 4.2 was used to dock the ligand with the targets. The target selected for docking was 3CE5 and 4B18. The results are visualized by Discovery Studio Visualizer 4.1. The results are compared with the standard drug N,N'-bis-(2-(1- piperidino)ethyl)-3,4,9,10-perylene tetracarboxylic acid diimide (PIPER).Results: From the results, butylamine derivative of perylene diimide possesses good binding energy when compared with standard drug PIPER. This result shows that the butylamine will be effective for anticancer therapy. In future, in vivo studies of butylamine derivative of perylene diimide will be carried out

APPLICATION OF IN SILICO STUDIES TARGETING TELOMERIC G-QUADRUPLEX COMPLEX BY PERYLENE DIIMIDES FOR ANTICANCER THERAPY

Objective: Telomerase enzyme which is expressed in detectable levels and its mechanism was that it increases the length when it binds to telomeres. This eventually leads to extension of lifespan of cells and also makes an attractive target for cancer therapy. Perylene diimides bind to telomerase with duplex genomic DNA, and these G-quadruplex ligands are of responsible for binding affinity with respective proteins. Based on the IC50 values of perylene diimides, QSAR has been studied out and the results are elaborated in preliminary research works. From the results of QSAR, the selected perylene ligands are selected for docking choosing telomerase as a target/protein. From the results of in silico studies, new compounds are designed and synthesized accordingly. Now, the objective of the study was to dock the final synthesized compounds with the telomerase protein to study regarding the pKi value using G-quadruplex ligand database (G4LDB). The docked results are visualized using Discovery Studio Visualizer 4.1. The results are compared with the standard N,N'-bis-(2-(1-piperidino)ethyl)-3,4,9,10-perylene tetracarboxylic acid diimide (PIPER) drug and these compounds will be effective for anticancer therapy.Methods: The study was to investigate the docking results of synthesized perylene compounds with the results from G4LDB and visualized by Discovery Studio 4.1 Visualizer. The telomerase proteins selected for the study were extracted from Protein Data Bank, and the proteins selected for the study are 3SC8 and 3CE5. Among the compounds (R1, R2, R3, and R4) screened in G-Quadruplex Ligand Database, compound R3 shows better binding affinity with good pKi value as well the interactions with the protein and ligand show better affinity with the targets and these are compared with the standard drug PIPER drug.Results: Compound R3 possesses the best binding affinity with the target 3CE5 and 3SC8 which shows that the compound will be effective for anticancer therapy

ENTERAL/ORAL GLUTAMINE SUPPLEMENTATION IN PATIENTS FOLLOWING SURGERY AND ACCIDENTAL INJURY

ABSTRACTObjective: The objective of this investigation was to study the effect of enteral/oral glutamine supplementation in patients following abdominalsurgery on plasma glutamine levels, rate of infection, and length of hospitalization (LOH).Methods: A randomized control trial was used, and the patients were randomly divided into two groups, namely experimental and control with30 participants each. Glutamine supplement (0.5 g/kg) was administered (oral and enteral) to the experimental group for 5 days post-surgeryimmediately after the feeding began. The study was conducted in ESIC hospital, Chennai, India.Results: The incidence of infection in the control group was found to be almost twice that in the experimental group considering the role of glutaminein combating infection. Furthermore, the LOH was found to be slightly higher in the control group as compared to the experimental group.Conclusion: This study has provided evidence that the supplementation of enteral glutamine in post-operative patients decreases the incidence ofpost-surgical infection, shortening of hospital stay and reduction in the overall hospital costs.Keywords: Glutamine supplementation, Post-operative patients, Oral and enteral feed

A PROSPECTIVE STUDY ON ROLE OF VITAMIN E SUPPLEMENTATION IN TYPE 2 DIABETES MELLITUS

Aim and Objective: The aim of the study was to evaluate the role of Vitamin E supplementation in Type II diabetes mellitus (DM), to determines whether people with Type II DM treated with hypoglycemic agents alone, with or without Vitamin E, to determines the drug interaction in such treatment regimen, and to evaluates the Safety of the regimen.Methods: Type II DM patients with or without complications were included in this study along with serum glycated hemoglobin (HbA1c) concentration between 7.5% and 9.5%. They are divided into test group (which received hypoglycemic agent along with Vitamin E 4000 IU) and control group. Body mass index (BMI) status, fasting blood sugar (FBS), and post-prandial blood sugar (PPBS) were noted once in a month, HbA1c percentage, total cholesterol level (TC), and serum Vitamin E level were estimated and noted for every 3 months at total 9 months of this study. Patients with other comorbid conditions were prominent in this study.Results: It is perceptible with the analysis of obtained data that FBS, PPBS, HbA1c percentage, TC level, and BMI status of the patients were declined gradually in test group (patients with Vitamin E supplementation along with their hypoglycemic agents). Thus, antioxidant therapy is highly propitious whereby delaying the onset of complications in patients with DM. This development would be highly helpful for diabetic patients

ANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF ATOMOXETINE HYDROCHLORIDE USING RAPID HIGH-PERFORMANCE LIQUID CHROMATOGRAPHIC TECHNIQUE

Objective: A simple, novel, sensitive, rapid high-performance liquid chromatographic (RP-HPLC) method has been developed and validated for quantitative determination of atomoxetine HCl (ATH) in bulk and formulations.Methods: The chromatographic development was carried out on RP-HPLC. The column used as Xterra RP 18 (250 mm × 4.6 mm, 5 μ particle size), with mobile phase consisting of methanol: water 80:20 V/V. The flow rate was 1.0 mL/min and the effluents were monitored at 270 nm.Results: The retention time was found to be 5.350 min. The method was validated as per International Conference on Harmonization Guideline with respect to linearity, accuracy, precision, and robustness. The calibration curve was found to be linear over a range of 2–10 μg/mL with a regression coefficient of 0.9999. The method has proved high sensitivity and specificity.Conclusion: The results of the study showed that the proposed RP-HPLC method was simple, rapid, precise and accurate which is useful for the routine determination of ATH in bulk drug and in its pharmaceutical dosage form

CLINICAL ASSOCIATION OF SERUM MAGNESIUM AND SERUM FIBRINOGEN LEVELS WITH ACUTE EXACERBATION OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE- A PROSPECTIVE OBSERVATIONAL STUDY

Objective: Acute exacerbations (AE) are a contributing cause of worsening chronic obstructive pulmonary disease (COPD) in conditions of lung function decline, quality of liveliness, and natural selection. The most important concept of this article is the positive correlation between the serum magnesium levels at worsening of symptoms and annual number of episodes. Methods: Blood samples from the patients who are diagnosed with AE of COPD will be collected and evaluated for serum magnesium levels and serum fibrinogen levels. Low serum magnesium is a modifiable risk factor. It is generally believed that, due to its bronchodilating effect, a decreased level of magnesium increases COPD exacerbations. The best blood biomarker for the systemic tenderness in COPD used here is plasma fibrinogen. Those with the increased fibrinogen levels had induced the higher admission rates with COPD. This clause deals with the association of both serum magnesium and serum fibrinogen levels with AE-COPD. Results: The serum magnesium levels on discharge in stable type were found to be 2.3±0.27, and in exacerbation, it was found to be 1.56±0.37. Moreover, on discharge, serum fibrinogen levels in stable type were found to be 1.64±0.32, and in exacerbation, it was found to be 2.18±0.40. Conclusion: Low serum magnesium levels may be a complication for AE of COPD. High serum fibrinogen levels may be a complication for AE of COPD. We hereby recommend regular screening of serum magnesium and serum fibrinogen levels for all the COPD patients to predict and prevent AE