Synthesis and antihistaminic activity of 3H-benzo [4,5] thieno [2,3-d][1,2,3] triazin-4-ones

AbstractIn the present study the antihistaminic activity of tricyclic benzothieno 1,2,3-triazine derivatives namely CP-3 (3-(phenyl)-5,6,7,8-tetrahydro,3H-benzo[4,5] thieno [2,3-d][1,2,3] triazin-4-one), CP-5 (3-(3-methyl phenyl)-5,6,7,8-tetrahydro,3H-benzo[4,5] thieno [2,3-d][1,2,3] triazin-4-one) and CP-8 (3-(4-chloro phenyl)-5,6,7,8-tetrahydro,3H-benzo[4,5] thieno [2,3-d][1,2,3] triazin-4-one) were evaluated using in vitro (isolated guinea pig ileum) and in vivo (bronchodilator activity in guinea pigs) models and the sedative potential of the test compounds were evaluated using actophotometer in mice. In in vitro antihistaminic study, the CP-3, CP-5, CP-8 and chlorpheniramine maleate (CPM) have shown a rightward shift in concentration response curve (CRC) of histamine with a change in EC50 values of histamine in all the four tissue preparations. The slope obtained in the schild plot indicated that CP-5, CP-8 and CPM were competitive in nature for H1-receptors. However, CP-3 has shown non-competitive antagonism. In in vivo antihistaminic study, the CP-3, CP-5, CP-8 and CPM have shown mean increase in exposition time against histamine challenge compared to control group (p<0.001). All the test drugs (10mg/kg) and CPM (2mg/kg) have offered a significant (p<0.001) protection against preconvulsive dyspnoea (PCD) compared to control. In conclusion, all the test drugs have shown very good antihistaminic activity and the test drugs have very little sedative action compared to CPM

Performance Evaluation of MANET Based Routing Protocols for VANETs in Urban Scenarios

Abstract. Vehicular Ad hoc NETworks (VANETs) are self-organizing ad hoc networks that are specifically designed for communication among vehicles where vehicles are themselves the nodes. Although routing protocols have already been analyzed and compared in the past for Mobile Ad hoc Networks (MANETs), simulations and comparisons of routing protocols for VANETs have almost always been done considering random motions with non-urban specific parameters. This paper studies the performance of Ad hoc On-Demand Distance Vector (AODV) and Destination Sequenced Distance Vector (DSDV) which are popular routing protocols in MANETS for routing among vehicular nodes in VANETs. The effects of urban motions on the simulation parameters, their consequences on routing performance are compared between the two protocols in this study. The VANET simulations showed that on-demand based protocol AODV performs better than the table-driven based DSDV protocol for two performance metrics for vehicular nodes moving in urban scenarios

Gastroprotective Properties of Karanjin from Karanja (Pongamia pinnata) Seeds; Role as Antioxidant and H+, K+-ATPase Inhibitor

Plant extracts are the most attractive sources of newer drugs and have been shown to produce promising results for the treatment of gastric ulcers. Karanjin, a furano-flavonoid has been evaluated for anti-ulcerogenic property by employing adult male albino rats. Karanjin (>95% pure) was administered to these rats in two different concentrations, that is, 10 and 20 mg kg−1 b.w. Ulcers were induced in the experimental animals by swim and ethanol stress. Serum, stomach and liver-tissue homogenates were assessed for biochemical parameters. Karanjin inhibited 50 and 74% of ulcers induced by swim stress at 10 and 20 mg kg−1 b.w., respectively. Gastric mucin was protected up to 85% in case of swim stress, whereas only 47% mucin recovery was seen in ethanol stress induced ulcers. H+, K+-ATPase activity, which was increased 2-fold in ulcer conditions, was normalized by Karanjin in both swim/ethanol stress-induced ulcer models. Karanjin could inhibit oxidative stress as evidenced by the normalization of lipid peroxidation and antioxidant enzyme (i.e., catalase, peroxidase and superoxide dismutase) levels. Karanjin at concentrations of 20 mg kg−1 b.w., when administered orally for 14 days, did not indicate any lethal effects. There were no significant differences in total protein, serum glutamate pyruvate transaminase, serum glutamate oxaloacetate transaminase and alkaline phosphatase between normal and Karanjin-treated rats indicating no adverse effect on major organs. During treatment schedule, animals remained as healthy as control animals with normal food and water intake and body weight gain

The Structure of the Phage T4 DNA Packaging Motor Suggests a Mechanism Dependent on Electrostatic Forces

SummaryViral genomes are packaged into “procapsids” by powerful molecular motors. We report the crystal structure of the DNA packaging motor protein, gene product 17 (gp17), in bacteriophage T4. The structure consists of an N-terminal ATPase domain, which provides energy for compacting DNA, and a C-terminal nuclease domain, which terminates packaging. We show that another function of the C-terminal domain is to translocate the genome into the procapsid. The two domains are in close contact in the crystal structure, representing a “tensed state.” A cryo-electron microscopy reconstruction of the T4 procapsid complexed with gp17 shows that the packaging motor is a pentamer and that the domains within each monomer are spatially separated, representing a “relaxed state.” These structures suggest a mechanism, supported by mutational and other data, in which electrostatic forces drive the DNA packaging by alternating between tensed and relaxed states. Similar mechanisms may occur in other molecular motors

Waste mangement- issues and solutions for a coastal village along Kerala, southwest coast of India

In the present world, plastics play an integral role in human life. Its production crosses 150 million tonnes per year globally and India contributes to more than 8 million tonnes, in terms of consumption. Plastic is cost effective, durable and holds a broad range of application, which turned it to a basic need for the human society. On the other side, 70 % of the consumption is converted as waste and when the infrastructure of the waste management system do not match with the generation rate, it becomes a menace to the society. One of the major concerns of fishermen has been the depleting fishery resources and degrading environment. With an aim to understand the magnitude of marine litter in coastal waters and the way it affects traditional small scale fishers the present study was undertaken. The study area is Mulavukad village Panchayat (latitude 10°02’98.21’’ and longitude 76°25’53.26’’) which is a long narrow stretch of land located in the Ernakulum district of Kerala state, India with an area of 19.27 sq km. The island is surrounded by Periyar river on the North east and Vembanad Lake on the South west. The major lively hood of the people is fishing and fishery related activities

Influence of selected anthropogenic impacts on ecology of Vembanad Lake

Influence of selected anthropogenic impacts on ecology of Vembanad Lak