Synthesis, and biological screening of chloropyrazine conjugated benzothiazepine derivatives as potential antimicrobial, antitubercular and cytotoxic agents

A series of twenty new chloropyrazine conjugated benzothiazepines (22-41) have been synthesized with 58%–95% yields. The compounds were characterized by using different spectroscopic techniques including FT-IR, ¹H NMR, ¹³C NMR spectroscopy and mass spectrometry. The synthesized compounds (22-41) and their precursor chalcones (2-21) were evaluated for antitubercular and cytotoxic activities. Additionally, compounds 22-41 were also tested for antimicrobial activity. Among the chalcone series (2-21), compounds 7 and 14 showed significant antitubercular activities (MICs 25.51 and 23.89 µM, respectively), whereas among benzothiazepines (22-41), compounds 27 and 34 displayed significant antimicrobial (MICs 38.02 µM, 19.01 µM) and antitubercular (MIC 18.10 µM) activities. Compounds 7 and 41 displayed cytotoxic activities with IC₅₀ of 46.03 ± 1 and 35.10 ± 2 µM respectively. All the compounds were evaluated for cytotoxic activity on normal human liver cell lines (L02) and found to be relatively less selective towards this cell line. The most active compounds identified through this study could be considered as potential leads for the development of drugs with possible antimicrobial, antitubercular, and cytotoxic activities

Fatty acid composition of serum and tissue lipids in male Indian desert gerbils (Meriones hurrianae; Jerdon) and Wistar rats

Serum lipids and fatty acid composition of total lipids, phospholipids and cholesterol ester fractions of serum, liver, heart and testes of male Indian desert gerbils (Marianas hurrianae; Jerdon) were analysed and compared with Wistar rats.Triglycerides in serum and liver were similar in gerbils and rats, Significant differences in the distribution of polyunsaturated fatty acids in different lipid fractions were observed between gerbils and rats. Total lipids, phospholipids and cholesterol  ester fractions in rats contained higher levels of arachidonic acid than in gerbils

AN M[X]/G/1M^{[X]}/G/1 QUEUE WITH OPTIONAL SERVICE AND WORKING BREAKDOWN

In this study, a batch arrival single service queue with two stages of service (second stage is optional) and working breakdown is investigated. When the system is in operation, it may breakdown at any time. During breakdown period, instead of terminating the service totally, it continues at a slower rate. We find the time-dependent probability generating functions in terms of their Laplace transforms and derive explicitly the corresponding steady state results. Furthermore, numerous measures indicating system performances, such as the average queue size and the average queue waiting time, has been obtained. Some of the numerical results and graphical representations were also presented

Antitubercular activity assessment of fluorinated chalcones, 2-aminopyridine-3-carbonitrile and 2-amino-4H-pyran-3-carbonitrile derivatives: In vitro, molecular docking and in-silico drug likeliness studies

A series of newer previously synthesized fluorinated chalcones and their 2-amino-pyridine-3-carbonitrile and 2-amino-4H-pyran-3-carbonitrile derivatives were screened for their in vitro antitubercular activity and in silico methods. Compound 40 (MIC~ 8 μM) was the most potent among all 60 compounds, whose potency is comparable with broad spectrum antibiotics like ciprofloxacin and streptomycin and three times more potent than pyrazinamide. Additionally, compound 40 was also less selective and hence non-toxic towards the human live cell lines-LO2 in its MTT assay. Compounds 30, 27, 50, 41, 51, and 60 have exhibited streptomycin like activity (MIC~16–18 μM). Fluorinated chalcones, pyridine and pyran derivatives were found to occupy prime position in thymidylate kinase enzymatic pockets in molecular docking studies. The molecule 40 being most potent had shown a binding energy of -9.67 Kcal/mol, while docking against thymidylate kinase, which was compared with its in vitro MIC value (~8 μM). These findings suggest that 2-aminopyridine-3-carbonitrile and 2-amino-4H-pyran-3-carbonitrile derivatives are prospective lead molecules for the development of novel antitubercular drugs

Corrosion and Tribological Characteristics of FSPed Aluminum Alloy AA5052

Friction stir processing (FSP) is a solid-state and effective process for surface modification of aluminium alloys. In this study the AA5052 alloy, widely used in marine applications, has been subjected to FSP. The FSP trials have been carried out by altering the FSP process parameters (tool rotation speed, tool traverse speed, and shoulder diameter). The friction stir processed specimens have been characterised / tested for microstructure, microhardness, sliding wear, immersion corrosion, and electrochemical corrosion. The hybrid polynomial – radial basis function-based models have been developed to determine the relationship between the process parameters and the evaluated properties. Furthermore, the optimum parameters for obtaining high hardness, wear resistance, and corrosion resistance have been determined. Microstructure evaluation in the friction stir processed specimens has shown refinement and uniform dispersion of β particles throughout the α-Al matrix. The results show that the improvement in properties is a result of the homogeneous dispersion of secondary β phase particles in the matrix. Friction stir processing of AA5052 alloy has improved hardness by ~14.5%, wear resistance by ~83%, and corrosion resistance ~87%. The optimum process window for friction stir processing of AA5052 alloy is tool rotation speed between 500 rpm and 900 rpm, tool traverse speed between 10 mm/min and 30 mm/min, and tool shoulder diameter of 18 mm and 21 mm

Self Controllable Health Care Monitoring Arrangement for Patient

In this undertaking is utilized to the Condition care monitoring system. Distributed Healthcare cloud computing arrangement considerably facilitates effectual patient treatment for health consultation by allocating confidential condition data amid healthcare providers. Though, it brings concerning the trial of keeping both the data confidentiality and patients’ individuality privacy simultaneously. Countless continuing admission manipulation and nameless authentication schemes cannot be straightforwardly exploited. The arrangement acts there are provider, doctor, patient and admin. The provider is list to website to consent staying to appeal dispatch to admin. Admin is Proved to in a particular provider it deeds to the present add to doctors and hospital divisions established. User or Patient is list to the site. Patient Login to present the deed booking the doctor appointment in situation patient to dispatch a feedback to that doctor treatment comments onward to admin. Doctors is add provider to dispatch a username and password .Doctor is login to think patient appointment features and checking the doctor is present patient or fake user to identified to dispatch to symptoms description upload files(x-ray).Admin is finished procedure is upheld in this system. Patient dispatch doctors feedback bad or wrong to particular doctors appointment annulled temporally. In this undertaking generally utilized for patient and hospital ,doctors features through online upheld for India astute established on card

Factors affecting landslide susceptibility mapping: Assessing the influence of different machine learning approaches, sampling strategies and data splitting

Data driven methods are widely used for the development of Landslide Susceptibility Mapping (LSM). The results of these methods are sensitive to different factors, such as the quality of input data, choice of algorithm, sampling strategies, and data splitting ratios. In this study, five different Machine Learning (ML) algorithms are used for LSM for the Wayanad district in Kerala, India, using two different sampling strategies and nine different train to test ratios in cross validation. The results show that Random Forest (RF), K Nearest Neighbors (KNN), and Support Vector Machine (SVM) algorithms provide better results than Naïve Bayes (NB) and Logistic Regression (LR) for the study area. NB and LR algorithms are less sensitive to the sampling strategy and data splitting, while the performance of the other three algorithms is considerably influenced by the sampling strategy. From the results, both the choice of algorithm and sampling strategy are critical in obtaining the best suited landslide susceptibility map for a region. The accuracies of KNN, RF, and SVM algorithms have increased by 10.51%, 10.02%, and 4.98% with the use of polygon landslide inventory data, while for NB and LR algorithms, the performance was slightly reduced with the use of polygon data. Thus, the sampling strategy and data splitting ratio are less consequential with NB and algorithms, while more data points provide better results for KNN, RF, and SVM algorithms

Stability analysis for yield and its attributing traits in advanced breeding lines of rabi sorghum (Sorghum bicolor (L.) Moench)

An experiment was carried out involving twenty three advanced breeding lines along with two checks M 35-1 and Muguthi during rabi season 2012-13 at four locations. Observations were recorded on 10 different characters viz., plant height (cm), stem diameter (cm), ear head length (cm), ear head diameter (cm), days to 50 per cent flowering, days to maturity, 100 seed weight (g), fodder yield per plot (kg), seed yield per plot (kg), and lodging percentage. The pooled analysis of variance revealed that mean sum of squares due to genotypes was significant for ear head diameter, days to 50 per cent flowering, days to maturity and fodder yield, indicating presence of considerable amount of variability in the genotypes. The mean sum of square due to environment + (genotypes x environment) was significant for plant height, ear head length (cm), ear head diameter (cm), days to 50 per cent flowering, fodder yield per plot (kg), seed yield per plot (kg), and lodging percentage characters except stem diameter, days to maturity and 100 seed yield. On the basis of stability parameters a four genotypes viz., GS-6 (2364 kg/ha), GS-16 (2454 kg/ha), GS-22(2775 kg/ha) and GS-23(2978 kg/ha) were found most stable over Gulbarga, Raichur, Bellary and Malnoor environments of Hyderabad Karnataka region

Character association and path analysis in advanced breeding lines of rabi sorghum [Sorghum bicolor (L.) Moench]

The field experiment was carried out using advanced breeding lines of rabi sorghum to study association among the yield and its component traits, direct and indirect effects of traits on the yield. Association studies indicated that seed yield per plot showed significant positive correlation with traits viz., plant height (rp=+0.7243, rg=+0.7409), ear head length (rp=+0.6002, rg=+0.6021), 100 seed weight (rp=+0.1593, rg=+0.1880), fodder yield (rp=+0.9434, rg=+0.9476) and lodging percentage (rp=+0.5263, rg=+0.5646) at both phenotypic and genotypic level.Genotypic correlation was higher magnitude than phenotypic correlation. Revealed increase in ear head length will increase the seed yield. Partitioning of yield and yield components both at phenotypic and genotypic levels into direct and indirect effects revealed that positive direct effects of ear head length (Ppi=+0.2533, Pgi=+0.5241), ear head diameter (Ppi=+0.0669, Pgi=+0.2580), days to maturity (Ppi=+0.0338, Pgi=+0.1193), fodder yield (Ppi=+0.6484, Pgi=+0.7461) were relatively high and followed by less lodging percentage (Ppi=+0.1751, Pgi=+0.2263). Residual effects were Pr=0.1303 and Gr=0.0624 at phenotypic and genotypic levels. Indicating importance of these characters and can be strategically used to improve the seed yield of sorghum