An Overview of Biological and Synthetic Aspects of Thiazole Derivatives in Heterocyclic Chemistry

These overviews signify a study covering the literature on thiazole derivatives in heterocyclic chemistry. This brief analysis as well provides a revise on current reports and demonstrates the utility and the effectiveness of this approach. The data on the process of synthesis, chemical reactions, and biological activity of these heterocycles available over the preceding years are assessing here. In the last few decades, a lot of effort has been prepared on thiazole ring to discover novel compounds associated to this scaffold. This review presents the advanced improvement on the proposed and growth of diverse thiazole derivatives. It is known as the building block in organic synthesis, which provides as an important outline for the improvement of diverse therapeutic agents and illustrate a broad variety of activities. These articles furnish a widespread explanation of the synthetic and biological value of thiazole engaged in the design and synthesis of diverse type of compounds encloses fused heterocyclic rings with more importance on latest literature

Synthesis and Screening of some benzoxazinone derivatives

Benzoxazinone derivatives fused with other heterocyclic and aromatic ring system were reported to possess various activities such as anti-inflammatory, analgesic, antimicrobial. The Benzoxazinone are an important group of secondary metabolites occurring in gramineae, acanthaceae, and ranunculaceae. Novel 1, 4-benzoxazin-3-one derivative have been synthesized which would have inhibitory activities against tyrosine kinases and the inhibitory activities against KDR and ABL which are closely related to chronic disease such as cancer. 1,4- Benzoxazinones has wide application in medicinal chemistry due to its pharmacological properties. The members of this family are used for treating parkinsons disease, ischemia reperfusion, selective potassium channel openers, antinociceptive, antidepressant and anti-fungal agent. Keywords: Benzoxazinone, secondary metabolites, tyrosine kinases, bantinociceptive

STABILITY INDICATING UPLC METHOD FOR QUANTIFICATION OF TOLPERISONE HCL AND PARACETAMOL FROM MUSCLE RELAXANT COMBINATION TABLET

Objective: In the present work, rapid and sensitive isocratic RP-UPLC method was established and comprehensive validation study for the estimation of Tolperisone HCl and Paracetamol was carried out according to international conference on harmonization (ICH) guidelines.Methods: Simultaneous estimation was chromatographed using 0.1% o-phosphoric acid in water and acetonitrile (70: 30 v/v) as a mobile phase at a flow rate of 0.20 ml/min with 35 ºC column temperature. Chromatographic separation accomplished isocratically on Acquity UPLC BEH C18 (50 mm ×2.1 mm, particle size 1.7 µm) and detection utilizing photodiode array detector at 254 nm. Injection volume was 2.0 µl.Results: The calibration curve was linear over the wide concentration range of 6.0µg/ml to 54.0µg/ml and 20.0µg/ml to 180.0µg/ml for Tolperisone HCl and Paracetamol, respectively. The retention time of Tolperisone HCl and Paracetamol was 1.396 and 2.625 min, respectively and the total analysis time was 5.0 min. Based on the results, the validated method was effectively applied for the estimation of Tolperisone HCl and Paracetamol in combined dosage form and in single pharmaceutical formulations with a new generation instrument, ultra performance liquid chromatography (UPLC). Moreover, the method helps to get better quality control and to pledge therapeutic efficacy.Conclusion: The method is simple, less time consuming and comparatively cost effective than existing methods.Â

Optimization for truss design using Bayesian optimization

In this work, geometry optimization of mechanical truss using computer-aided finite element analysis is presented. The shape of the truss is a dominant factor in determining the capacity of load it can bear. At a given parameter space, our goal is to find the parameters of a hull that maximize the load-bearing capacity and also don't yield to the induced stress. We rely on finite element analysis, which is a computationally costly design analysis tool for design evaluation. For such expensive to-evaluate functions, we chose Bayesian optimization as our optimization framework which has empirically proven sample efficient than other simulation-based optimization methods. By utilizing Bayesian optimization algorithms, the truss design involves iteratively evaluating a set of candidate truss designs and updating a probabilistic model of the design space based on the results. The model is used to predict the performance of each candidate design, and the next candidate design is selected based on the prediction and an acquisition function that balances exploration and exploitation of the design space. Our result can be used as a baseline for future study on AI-based optimization in expensive engineering domains especially in finite element Analysis

Squeezing Problems in Indian Tunnels

Case histories of three Indian tunnels indicate that squeezing conditions are created due to plastic flow of rock masses under the influence of high cover pressures. These examples emphasize that a tunnel experiencing squeezing conditions must be allowed to deform to optimize support costs and avoid delays. Allowance for desirable tunnel deformations must, therefore, be made while planning the size of excavation. Field data has shown that a flexible support system of compressible backfill and steel ribs may be used as an alternative to shotcrete support which is unpractical in Indian tunnels excavated largely by conventional methods. Instrumentation indicates that large broken zones are associated with late stabilization and that the coefficient of volumetric expansion of failed rock masses is significantly lower than believed so far. Comparison of measured rock pressures with those estimated from available methods shows that the elasto-plastic theory may provide reliable predictions provided that the strength parameters of rock masses are known precisely

Stability of Suspension Bridge Anchorage System

The lift side anchor system for a 151 m span suspension bridge over river Alaknanda in Himalayan region was unstable. The gravity type anchor block for the suspension bridge was constructed by cutting the toe of the natural slope. Walls were constructed to retaining the backfill and the anchor block. Slips along the natural slope were frequent. The site lies in an active seismic zone. The paper presents the details of analysis of anchor block, retaining walls and the natural slopes. The analysis is carried out both under static condition and also by taking seismic coefficients. The already constructed retaining walls which were unsafe have been strengthened by designing a composite retaining wall keeping in view the requirements of the client not to demolish any of the already constructed retaining wall

Damage and Remedial Measures for Buildings on Hill Slopes

The paper deals with details of geotechnical investigations carried out for evaluating the reasons of damage to the buildings resting on hill slopes in northern region of India and also to evaluate the soil parameters for designing retaining walls and other remedial measures for preventing further damage to structures. Three causes of failure were identified namely (i) instability of slopes, (ii) improper design of retaining walls and (iii) differential settlement of structures. Shear strength parameters of the soil mass required for the analysis of slope stability and stability of retaining wall sections have been chosen based on three methods of investigations viz. large scale direct in-situ shear tests, plate load tests and the back analysis method. The stability analysis of various sections of slopes have been carried out and measures for strengthening of slopes have been suggested

A study on clinical profile of patients presenting with adverse drug reaction: a hospital based prospective observational study

Background: The aim of the study was to study the clinical profile of patients presenting with adverse drug reaction.Methods: The study was conducted in the Department of Medicine, IGMC Shimla from 01 July 2015 to 30 June 2016. A total of 129 patients were included in this study. A detailed history was taken followed by examination of patients. The routine investigations were done and special investigations as per need. For analysis patients detail, suspected drugs and the adverse drug reactions caused by them were used.Results: Bleeding from various sites was the most common event (39.5%), followed by symptomatic hypoglycemia 22.5% of events and symptomatic hyponatremia in 16.3% events. Amongst various drug classes anticoagulants were the most commonly involved drug class followed by oral hypoglycaemic agents, diuretics and antiplatelets. Type A was predominant ADR constituting (97.7%) of total ADRs and only (2.3%) of ADRs were of type B. After causality assessment, majority 86 (66.6%) were probable related and large number 127 (98.3%) of ADRs were serious which recovered after hospitalization.Conclusions: Our study revealed that ADRs are frequent and are easily recognized in clinical practice and are mostly preventable. Most ADRs are due to the use of drugs with high toxicity for example, warfarin often results in bleeding. It also shows that careful drug monitoring in hospitals  may lead to reduction of many such ADRs, suggesting that some type A, ADRs may be due to inadequate monitoring of therapies and doses. This study will aid the development of interventions to reduce the impact of ADRs in hospital in-patients

Stability of Slopes - A Case History

A Lecture cum-cinema hall was constructed on a terrace developed at the top of a hillock at a site located in the north-eastern part of India. At the time of development of the site, excavated soil was dumped on the slopes and retaining walls were constructed to retain the earth. After the first monsoon, the retaining walls gave way. Further distress in the vicinity of the building was noticed in the subsequent three years. The paper describes the details of the above failure, the investigations carried out and the remedial measures suggested

Synthesis and evaluation of novel analogues of mangiferin as potent antipyretic

ObjectiveTo screen different analogues of mangiferin pharmacologically for antipyretic activity.MethodsThe naturally occurring xanthone glycoside mangiferin was isolated by column chromatography from the ethanolic extract of stem bark of Mangifera indica. Mangiferin was further converted to 5–(N–phenylamino methyleno) mangiferin, 5–(N–p–chlorophenylamino methyleno) mangiferin, 5–(N–2-methyl phenylamino methyleno) mangiferin, 5–(N–p–methoxy phenylamino methyleno) mangiferin, 5–(N, N–diphenylamino methyleno) mangiferin, 5–(N–α–napthylamino methyleno) mangiferin and 5–(N–4–methyl phenylamino methyleno) mangiferin analogues. The synthesized compounds were further screened for antipyretic activity along with mangiferin at a dose level of 100 and 200 mg/kg. Mangiferin and its analogues were characterized by melting point andRfvalue determination and through spectral technique like UV, IR, and NMR spectral analysis.ResultsThe antipyretic activity of mangiferin as well as all analogues was found to be more significant in at higher dose ie. 200 mg/kg which was depicted through a decrease in rectal temperature up to 3 h.ConclusionsThe antipyretic activity of mangiferin and its analogues may be attributed to inhibition in synthesis of TNF–α and anti-oxidant activity associated with amelioration of inflammatory actions of cytokines