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

First report of the occurrence of Myrothecium verrucaria in watermelon seeds from India

Watermelon (Citrullus lanatus) is known to be affected by a variety of both seed-borne and soil-borne fungi. In routine screening of watermelon seed samples, sporodochia of Myrothecium verrucaria were observed. The fungus was isolated and the spore suspension was inoculated onto healthy seedlings of watermelon. The resulting symptoms confirmed Koch's postulates

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

SCREENING OF MULTI BIOACTIVE METABOLITES PRODUCING MICROORGANISMFROM GARDEN SOIL OF DR. M. G. R EDUCATIONAL AND RESEARCH INSTITUTE, CHENNAI

Objective: Screening of industrial important bioactive metabolites of Antibiotics, hydrolytic enzymes producing microorganism from garden soil of Dr. M. G. R Educational and Research Institute, Chennai. Methods: Desired ten soil samples taken and were serially diluted. Crowded plate method used for antibiotic-producing microorganism and Starch agar medium and gelatin medium tests were performed for hydrolytic enzymes (Amylase and Gelatinase). Results: Among the tested soil samples, antibiotic producing microorganisms were not found, but has hydrolytic enzymes amylase and gelatinase. Thus screened soil samples biochemically identified as Bacillus species. Conclusion: This study concludes that, the collected sample, produced Antibiotic negative result and it’s possess other industrial important hydrolytic enzymes. Thus Screening of more bioactive metabolites producing ability from a single isolate, will be more useful for effective screening

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

Probing the Role of Magnetic-Field Variations in NOAA AR 8038 in Producing Solar Flare and CME on 12 May 1997

We carried out a multi-wavelength study of a CME and a medium-size 1B/C1.3 flare occurring on 12 May 1997. We present the investigation of magnetic-field variations in the NOAA Active Region 8038 which was observed on the Sun during 7--16 May 1997. Analyses of H{\alpha} filtergrams and MDI/SOHO magnetograms revealed continual but discrete surge activity, and emergence and cancellation of flux in this active region. The movie of these magnetograms revealed two important results that the major opposite polarities of pre-existing region as well as in the emerging flux region (EFR) were approaching towards each other and moving magnetic features (MMF) were ejecting out from the major north polarity at a quasi-periodicity of about ten hrs during 10--13 May 1997. These activities were probably caused by the magnetic reconnection in the lower atmosphere driven by photospheric convergence motions, which were evident in magnetograms. The magnetic field variations such as flux, gradient, and sunspot rotation revealed that free energy was slowly being stored in the corona. The slow low-layer magnetic reconnection may be responsible for this storage and the formation of a sigmoidal core field or a flux rope leading to the eventual eruption. The occurrence of EUV brightenings in the sigmoidal core field prior to the rise of a flux rope suggests that the eruption was triggered by the inner tether-cutting reconnection, but not the external breakout reconnection. An impulsive acceleration revealed from fast separation of the H{\alpha} ribbons of the first 150 seconds suggests the CME accelerated in the inner corona, which is consistent with the temporal profile of the reconnection electric field. In conclusion, we propose a qualitative model in view of framework of a solar eruption involving, mass ejections, filament eruption, CME, and subsequent flare.Comment: 8 figures, accepted for publication in Solar Physic

High activity redox catalysts synthesized by chemical vapor impregnation

The use of precious metals in heterogeneous catalysis relies on the preparation of small nanoparticles that are stable under reaction conditions. To date, most conventional routes used to prepare noble metal nanoparticles have drawbacks related to surface contamination, particle agglomeration, and reproducibility restraints. We have prepared titania-supported palladium (Pd) and platinum (Pt) catalysts using a simplified vapor deposition technique termed chemical vapor impregnation (CVI) that can be performed in any standard chemical laboratory. These materials, composed of nanoparticles typically below 3 nm in size, show remarkable activity under mild conditions for oxidation and hydrogenation reactions of industrial importance. We demonstrate the preparation of bimetallic Pd–Pt homogeneous alloy nanoparticles by this new CVI method, which show synergistic effects in toluene oxidation. The versatility of our CVI methodology to be able to tailor the composition and morphology of supported nanoparticles in an easily accessible and scalable manner is further demonstrated by the synthesis of Pdshell–Aucore nanoparticles using CVI deposition of Pd onto preformed Au nanoparticles supported on titania (prepared by sol immobilization) in addition to the presence of monometallic Au and Pd nanoparticles

Relationships between Parental Education and Overweight with Childhood Overweight and Physical Activity in 9-11 Year Old Children: Results from a 12-Country Study

Background: Globally, the high prevalence of overweight and low levels of physical activity among children has serious implications for morbidity and premature mortality in adulthood. Various parental factors are associated with childhood overweight and physical activity. The objective of this paper was to investigate relationships between parental education or overweight, and (i) child overweight, (ii) child physical activity, and (iii) explore household coexistence of overweight, in a large international sample. Methods: Data were collected from 4752 children (9-11 years) as part of the International Study of Childhood Obesity, Lifestyle and the Environment in 12 countries around the world. Physical activity of participating children was assessed by accelerometry, and body weight directly measured. Questionnaires were used to collect parents' education level, weight, and height. Results: Maternal and paternal overweight were positively associated with child overweight. Higher household coexistence of parent-child overweight was observed among overweight children compared to the total sample. There was a positive relationship between maternal education and child overweight in Colombia 1.90 (1.23-2.94) [odds ratio (confidence interval)] and Kenya 4.80 (2.21-10.43), and a negative relationship between paternal education and child overweight in Brazil 0.55 (0.33-0.92) and the USA 0.54 (0.33-0.88). Maternal education was negatively associated with children meeting physical activity guidelines in Colombia 0.53 (0.33-0.85), Kenya 0.35 (0.19-0.63), and Portugal 0.54 (0.31-0.96). Conclusions: Results are aligned with previous studies showing positive associations between parental and child overweight in all countries, and positive relationships between parental education and child overweight or negative associations between parental education and child physical activity in lower economic status countries. Relationships between maternal and paternal education and child weight status and physical activity appear to be related to the developmental stage of different countries. Given these varied relationships, it is crucial to further explore familial factors when investigating child overweight and physical activity

Improved risk stratification of patients with atrial fibrillation: an integrated GARFIELD-AF tool for the prediction of mortality, stroke and bleed in patients with and without anticoagulation.

OBJECTIVES: To provide an accurate, web-based tool for stratifying patients with atrial fibrillation to facilitate decisions on the potential benefits/risks of anticoagulation, based on mortality, stroke and bleeding risks. DESIGN: The new tool was developed, using stepwise regression, for all and then applied to lower risk patients. C-statistics were compared with CHA2DS2-VASc using 30-fold cross-validation to control for overfitting. External validation was undertaken in an independent dataset, Outcome Registry for Better Informed Treatment of Atrial Fibrillation (ORBIT-AF). PARTICIPANTS: Data from 39 898 patients enrolled in the prospective GARFIELD-AF registry provided the basis for deriving and validating an integrated risk tool to predict stroke risk, mortality and bleeding risk. RESULTS: The discriminatory value of the GARFIELD-AF risk model was superior to CHA2DS2-VASc for patients with or without anticoagulation. C-statistics (95% CI) for all-cause mortality, ischaemic stroke/systemic embolism and haemorrhagic stroke/major bleeding (treated patients) were: 0.77 (0.76 to 0.78), 0.69 (0.67 to 0.71) and 0.66 (0.62 to 0.69), respectively, for the GARFIELD-AF risk models, and 0.66 (0.64-0.67), 0.64 (0.61-0.66) and 0.64 (0.61-0.68), respectively, for CHA2DS2-VASc (or HAS-BLED for bleeding). In very low to low risk patients (CHA2DS2-VASc 0 or 1 (men) and 1 or 2 (women)), the CHA2DS2-VASc and HAS-BLED (for bleeding) scores offered weak discriminatory value for mortality, stroke/systemic embolism and major bleeding. C-statistics for the GARFIELD-AF risk tool were 0.69 (0.64 to 0.75), 0.65 (0.56 to 0.73) and 0.60 (0.47 to 0.73) for each end point, respectively, versus 0.50 (0.45 to 0.55), 0.59 (0.50 to 0.67) and 0.55 (0.53 to 0.56) for CHA2DS2-VASc (or HAS-BLED for bleeding). Upon validation in the ORBIT-AF population, C-statistics showed that the GARFIELD-AF risk tool was effective for predicting 1-year all-cause mortality using the full and simplified model for all-cause mortality: C-statistics 0.75 (0.73 to 0.77) and 0.75 (0.73 to 0.77), respectively, and for predicting for any stroke or systemic embolism over 1 year, C-statistics 0.68 (0.62 to 0.74). CONCLUSIONS: Performance of the GARFIELD-AF risk tool was superior to CHA2DS2-VASc in predicting stroke and mortality and superior to HAS-BLED for bleeding, overall and in lower risk patients. The GARFIELD-AF tool has the potential for incorporation in routine electronic systems, and for the first time, permits simultaneous evaluation of ischaemic stroke, mortality and bleeding risks. CLINICAL TRIAL REGISTRATION: URL: http://www.clinicaltrials.gov. Unique identifier for GARFIELD-AF (NCT01090362) and for ORBIT-AF (NCT01165710)