Purpose of the study. We aimed to find and study in silico and in vivo novel thienopyridine and dihydropyridine derivatives with hypoglycemic activity. Materials and methods. Three derivatives of thienopyridine and dihydropyridine with potential hypoglycemic effect were selected from 350 novel cyanothioacetamide derivatives synthesized by the authors in the “ChemEx” Research Laboratory using virtual bioscreening based on SwissTargetPrediction software, and their oral administration safety was assessed. During the experimental study conducted on 72 mature male Wistar rats, we modeled hyperglycemia in the animals by means of high-fat diet and dexamethasone load, then we performed pharmacological correction of metabolic disorders with the novel compounds and comparison drugs - Metformin, Vildagliptin. Upon withdrawal of animals from the experiment, blood was sampled for further biochemical investigation and determination of glucose concentration, ALT, AST, total bilirubin, triglycerides, and total blood cholesterol levels. Results. The results of molecular docking showed that the novel compounds with the codes AZ-383, AZ-257, and AZ-020 have putative effects on biotargets with potential for the correction of hyperglycemia and positive impact on lipid metabolism and liver function. In addition, these compounds have a good safety profile when administered orally. In the in vivo study, compounds AZ-383, AZ-257, and AZ-020 were found to have hypoglycemic activity and associated hepatoprotective and hypolipidemic properties. Conclusions. Novel derivatives of thienopyridine and dihydropyridine showed hypoglycemic activity in the experiment following metabolic disorder modeling in animals. This corresponds fully with the biotargets identified in silico for these compounds. Pharmacological activity of compounds with the codes AZ-383, AZ-257, and AZ-020, as well as their oral administration safety confirm the high relevance of further study.
Abstract: The future generation of wireless system is expected to provide multi class services, multimedia at any time anywhere with seamless mobility and Quality of Service (QoS). In such environment, optimal vertical handoff is a challenging issue. Unnecessary handoff causes wastage of network resources and thus affects the QoS of network. To reduce the handoff, in this paper, a Modified Cat Swarm Behavior based Optimization (MCSBO) based handoff algorithm is proposed in heterogeneous wireless mobile network. Initially, resource-poor mobile nodes, and resource-rich mobile nodes are clustered using Modified Expectation Maximization (MEM) to reduce the handoffs efficiently. Here, parameters like packet loss rate, dynamic new calls blocking probability, Bandwidth, and Cost along with the velocity of the Mobile Terminal (MT) are considered for the design of the Handoff algorithm. The Membership Functions (MFs) for each of the parameter are determined and corresponding Membership Degrees are evaluated from their concerned MFs. The optimized fuzzification of the parameters is obtained via developing the appropriate weight vector. The weight vector is optimized using MCSBO algorithm. Experimental results show that the proposed algorithms attained best performance bandwidth utilization, handoff dropping rate and handoff rate compared to existing handoff decision vector algorithms.
Bioremediation of pesticides is imperative for a sustainable environment. For this purpose soil borne, pure fungal strains; Aspergillus niger and Penicillium chrysogenum were augmented in soils spiked with herbicide, Chlorsulfuron from four distinct regions of Pakistan. These strains were found to utilize Chlorsulfuron as their carbon and energy sources. Solid-liquid extraction of pesticide was followed by analysis through high performance liquid chromatography and gas chromatography mass spectrometry-SIM (selected ion monitoring mode). The use of chromatographic techniques for analysis of Chlorsulfuron and its transformation products is of paramount importance. The SIM mode enhanced the sensitivity of GCMS momentously, subsequently distinguishing chemicals even in lower detection limits. Chemical hydrolysis experiments, performed on the same soils were also found to degrade Chlorsulfuron (50%) but to a lesser extent than biodegradation (76 and 74% by both strains). Degradation rate followed first order reaction kinetics. Two major metabolites were obtained after degradation; 2-chlorobenzenesulfonamide and 2-amino-4-methoxy-6-methyl-1,3,5-triazine. Aspergillus niger degraded Chlorsulfuron (76%) slightly more than Penicillium chrysogenum (74%). R2 for degradation rates for all soil samples by both fungal strains were close to 1 and P values were less than 0.05, indicating significance of results.
In the last two decades, major car manufacturing companies are exploring the possibilities of joining magnesium with aluminium, via friction welding technique for many crucial automotive applications. Our primary objective, an experimental investigation has been carried out to study the behaviour of dissimilar joints. The microscopic structure at the welded joint interface was analysed using an optical microscopy and scanning electron microscope. It was found that, by increasing the value of friction time, the value of the tensile strength increases and the result of tensile strength is found to be 120 MPa at a friction time of 10 secs. Micro hardness was found to be higher at the interface of the weldment due to the development of a brittle intermetallic compound. Micro structural studies using SEM reveals, distinct zones such as an unaffected parent metal zone, the heat affected zone, a thermo-mechanically affected zone and a fully deformed plasticised zone.
This paper proposes use of high gain Negative self lift luo DC-DC converter to step up the low voltage from PV panel and fed to microgrid system as in marine ships to reduce to demand on fossil fuels and carbon emission control. Negative luo converter has the advantage of smaller size, weight, high frequency switching and stable output over positive luo converters and traditional Boost converters. In this paper the comparison of positive and negative luo converter is done and based on the results, negative output is concluded based on performance.
SS 430 thin plates are extensively used in medical equipment, decorative products and kitchen appliances. In this research work, the 16 straight cutting profiles on SS 430 plates were done by using Nd:YAG laser cutting processes. Experimental works were conducted to examine the influence of processing conditions of laser cutting such as power, cutting velocity and gas pressure on response characteristics like HAZ (heat affected zone) size, recast layer thickness and micro hardness. A novel integrated Taguchi-entropy weighted based Grey relational analysis (GRA) approach has been employed to attain the supreme qualities of laser cutting in this effort. The entropy method is used to measure the weight to each response characteristics. Additionally, ANOVA technique is used to identify the significant process parameters. The obtained results point out that these approaches convincing to optimize the laser cutting practices.
This article presents a new approach to compensation for manufacturing errors in real time. This approach is based on the insertion of the mathematical models into a G-code form in NC programming. Compensated errors in this work are errors due to cutting tool wear, errors due to tool path, and errors due to positioning. We used the lagrange method to model errors due to the trajectory and wear of the cutting tool and the small displacement method for positioning.
The purpose of this study was to examine the effects of warm-up intensity on total oxygen uptake and VO2 kinetics (time constants) during sub¬¬¬maximal exercise in the Iranian national female futsall player’s. The participants of this study were ten Players of Iranian futsal national team (mean± SD: age,22.5±3.2yrs;weight,56.04±6.17kg;height,163±3.68cm;bodyfat%,23.5±3.8;BMI, 21.07± 2.22kg/m2; VO2max, 46.05± 4.61 ml.kg-1.min-1 ). After measuring of VO2max and LT in first session, the subjects performed two protocols of warm up (moderate and heavy intensity) and one protocol with¬out warm up before sub¬maximal exercise (80%LT) in three separated sessions. Respiratory gas exchange measured by Gas Analyzer during the exercise. Repeated measures ANOVA and LSD test were applied for statistical analysis. Total oxygen uptakes were not significant difference after three conditions. After moderate and heavy warm up, third time constants significantly reduced in compare to with¬out warm-up (p<0/05). also oxygen uptake/time ratio in third time constants significantly increased after moderate and heavy warm up respect to with¬out warm-up (p<0/05). The results suggest that warm up causes reducing the time of reaching to steady state of O2 uptake in sub maximal exercise and this effect is independent to warm up intensity.