Synthesis of 1-Substituted-4-(Pyridin-4-yl) [1,2,4] Triazolo [4,3-a] Quinazolin-5(4H)-ones as a New Class of H1- Antihistaminic Agents

Purpose: To synthesize a new series of 1-substituted-4-(pyridin-4-yl) [1,2,4] triazolo [4,3-a]quinazolin- 5(4H)-ones and evaluate them for H1-antihistaminic activity with negligible side effects in guinea pigs.Methods: The synthesized compounds were characterized by Infrared spectroscopy (IR), proton nuclear magnetic resonance (1H-NMR) and mass spectrometry (MS) data. The purity of the compounds was determined by elemental analysis. The antihistaminic activity of the compounds was evaluated in guinea pigs by histamine-induced bronchoconstriction method.Results: Among the series, 1-methyl-4-(pyridin-4-yl) [1,2,4] triazolo [4,3-a] quinazolin-5(4H)-one (S5) was the most potent with 72.85 % protection and its potency was comparable to that of the reference, chlorpheniramine maleate (70.09 %). Interestingly, the sedative property of compound S5 was negligible (5.09 %) when compared to chlorpheniramine maleate (29.58 %).Conclusion: Compound S5 can serve as a lead molecule for further development into a new class of H1-antihistaminic agents.Keywords: Quinazolin-5-ones, Antihistaminic activity, Histamine, Bronchoconstrictio

IN VITRO EVALUATION OF ANTHELMINTIC ACTIVITY OF AQUEOUS EXTRACT OF ARDISIA COLORATA ROXB. LEAVES IN ADULT EARTHWORMS

Objective: The study aims to evaluate the anthelmintic activity of aqueous extract of Ardisia colorata Roxb. leaves (AQEAC) using adult earthworms (Pheretima posthuman). Methods: The total of 24 adult earthworms were divided into four groups, with six worms in each group (n=6). The anthelmintic activity of AQEAC at two different doses (25 mg/ml and 50 mg/ml) was evaluated by assessing the time of paralysis (min) and time of death (min) of the earthworms. Albendazole (25 mg/ml) was used as standard and 2% gum acacia as control. Results: The result showed that AQEAChad significant anthelmintic activity (p<0.001) in a dose-dependent manner but was less potent than the standard drug albendazole. Conclusion: AQEAC demonstrated significant anthelmintic activity but was less potent than the standard drug albendazole. However, further studies with higher doses are required to evaluate the dose-dependent activity and to evaluate the exact mechanism responsible for anthelmintic activity

An Internet Based Framework for Micro Devices Assembly

ABSTRACT This paper outlines the design of an Internet based collaborative framework to support the rapid assembly of micro devices. With the help of an agent programming language called 3APL, a distributed approach to achieving the life cycle of the various phases in the assembly of micro devices has been implemented. A discussion of the various agent resources created for a VE oriented approach is also provided in this paper

The Effects of Nano Fillers on Space Charge Distribution in Cross-Linked Polyethylene

The performance of polymeric insulation will be distorted by the accumulation of space charge. This will lead to local electric field enhancement within the insulation material that can cause degradation and electrical breakdown. The introduction of nanofillers in the insulation material is expected to reduce the space charge effect. However, there is a need to analyze potential nanofillers to determine the best option. Therefore, the objective of this research work is to examine two types of nanofillers for Cross-Linked Polyethylene (XLPE); Zinc Oxide (ZnO) and Acrylic (PA40). The effects of these nanofillers were measured using the Pulsed-Electro Acoustic (PEA) method. The development of space charge is observed at three different DC voltage levels in room temperature. The results show that hetero charge distribution is dominant in pure XLPE materials. The use of both nanofiller types have significant effect in decreasing the space charge accumulation. With nanofillers, the charge profile changed to homo-charge distribution, suppressing the space charge formation. Comparisonbetween both the nanofillers show that PA40 has better suppression performance than ZnO

Variability in quality attributes of paprika and paprika alike chillies (Capsicum annuum L.)

An investigation was carried out to assess the variability in paprika alike chillies (26 indigenous germplasm) and paprika lines (18 exotic collections) for yield and quality attributing parameters, which would inturn help in identifying and utilizing the promising lines for crop improvement. Highly significant variation was recorded among the genotypes for yield and quality contributing characters. Kt-Pl-19, Kt-Pl-19 variant–I, ICBD-10, ICBD-8, SSP-1999 and PBC-171, were found promising, while ICBD-10, ICBD-8, ICBD-1, ICBD-11, ICBD-6, ICBD-19, CC-1, EC-171, EC-490, EC-18, EC-6, EC-45, EC-71 and EC-14 proved to be ideal for quality attributes. Based on yield and quality parameters, the genotypes ICBD-10, ICBD-8 and EC-18 were found suitable for paprika industry with high yield (> 850 g plant–1) and high quality attributing characters (> 200 ASTA units and < 0.5% capsaicin). Among the various characters, maximum coefficient of variation (15.25%) was recorded for capsaicin content in both indigenous and exotic germplasm and minimum variation for color value (0.46%) in the indigenous germplasm and weight of pericarp (6.78%) in the exotic collections. &nbsp

Variability and character association in paprika and paprika alike chillies

An experiment was conducted to estimate variability and character association in a set of 25 indigenous (paprika alike chillies) and 18 exotic (paprika) germplasm of paprika. Wide range of variation was observed for all the characters except for capsaicin content, weight of seeds, fruit girth and length. The maximum range of variation was recorded for yield plant-1 followed by color value, plant height and number of seeds fruit-1. Among the various traits, maximum coefficient of variation was observed for capsaicin content, followed by weight of pericarp fruit-1, yield plant-1 and weight of seeds fruit-1 in the indigenous lines of paprika. Similarly, in the exotic and combined germplasm of paprika and paprika alike chillies, maximum range of variation was registered with yield plant-1, followed by color value, number of seeds fruit-1 and plant height and narrow range of variation was observed with capsaicin content. In the combined germplasm, maximum coefficient of variation was recorded with capsaicin content, followed by weight of pericarp fruit-1, yield plant-1 and color value. Weight of pericarp, number and weight of seeds fruit-1 were identified as important yield components and selection should be focused on these traits for improvement of paprika and paprika alike chillies. &nbsp

Cluster analysis based on biochemical constituents in paprika like chillies (Capsicum annuum L.)

Chillies and paprika like chillies (Capsicum annuum L.) belonging to Solanaceae, is a source of natural colour, widely used in the food industry and is in great demand in the international market. Twenty-four accessions belonging to Indigenous Collections of Byadagi Dabbi (ICBD) and others were analyzed for biochemical constituents from leaf. Biochemical constituents studied were total carbohydrate, starch, reducing sugars, total free amino acids, phenol and protein. The accessions were compared for the isozymes viz., peroxidase, super oxide dismutase and poly phenol oxidase in the leaf, besides, leaf protein using SDS-PAGE. The dendrogram showing the relationship among the accessions for leaf biochemical constituents and colour value of fruits formed six clusters. Colour value ranged from 109 to 353 ASTA units. The accessions ICBD-11 and ICBD-19 possessed highest colour value. Accession ICBD-24 was distinctly different from others. Accessions in each cluster had almost uniform colour value and uniform isozyme profile. The accession ICBD-24 was a Coorg collection and ICBD-11 and ICBD-19 were from Dharwad district of Karnataka. Significant positive correlation was observed between colour value and total free amino acids, total protein, total phenol and polyphenol oxidase in paprika like chillies. &nbsp

Lightweight Self-Compacting Concrete Incorporating Industrial Rejects and Mineral Admixtures: Strength and Durability Assessment

By the recent global research developments, a lot of natural and artificial materials that are normally discarded and landfilled, are continually investigated for potential construction applications. In this study, the mechanical and durability properties of lightweight self-compacting concrete produced using pumice, ground granulated blast furnace slag (GGBS), rice husk ash (RHA) and precipitated silica, was investigated. A detailed experimental design was performed, which entailed reducing the water powder ratio, and use of viscosity modifying admixture, for enhancing the fresh SCC quality. The experimental process involved assessment of mechanical and durability properties of concrete mixtures. The results have shown that compressive and flexural strength of SCC made with lightweight aggregate are improved using mineral blended cement. Also, same mix, but with pumice as coarse aggregate gave higher split-tensile strength than other mixtures. This study deduced that pozzolanic reactivity and filler action of supplementary cementitious materials used, enhanced the resistance of the mixtures to deterioration when exposed to aggressive environment

Disturbances in Hypothalamic-Pituitary-Adrenal Axis and Immunological Activity Differentiating between Unipolar and Bipolar Depressive Episodes

Differentiating bipolar depression (BD) from unipolar depression (UD) is difficult in clinical practice and, consequently, accurate recognition of BD can take as long as nine years. Research has therefore focused on the discriminatory capacities of biomarkers, such as markers of the hypothalamic-pituitary-adrenal (HPA) axis or immunological activity. However, no previous study included assessments of both systems, which is problematic as they may influence each other. Therefore, this study aimed to explore whether cortisol indicators and inflammatory markers were a) independently associated with and/or b) showed effect modification in relation to a lifetime (hypo)manic episode in a large sample of depressed patients.Data were derived from the Netherlands Study of Depression and Anxiety and comprised 764 patients with a DSM-IV depressive disorder at baseline, of which 124 (16.2%) had a lifetime (hypo)manic episode at the 2-year assessment, or a more recent episode at the 4-year or 6-year assessment. Baseline cortisol awakening response, evening cortisol and diurnal cortisol slope were considered as cortisol indicators, while baseline C-reactive Protein (CRP), Interleukin-6 (IL-6), and Tumor Necrosis Factor Alpha (TNF-α) were included as inflammatory markers.In depressed men and women, none of the cortisol indicators and inflammatory markers were (independently) associated with a (hypo)manic episode. However, effect modification was found of diurnal cortisol slope and CRP in relation to a (hypo)manic episode. Further analyses showed that depressed men with high levels of diurnal cortisol slope and CRP had an increased odds (OR=10.99, p=.001) of having a (hypo)manic episode. No significant differences were found in women.Our findings suggest that the combination of high diurnal cortisol slope and high CRP may differentiate between UD and BD. This stresses the importance of considering HPA-axis and immunological activity simultaneously, but more research is needed to unravel their interrelatedness