Pharmacological evaluation and preparation of nonsteroidal anti-inflammatory drugs containing an N-Acyl hydrazone subunit

A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a–e) were synthesized and characterized. Docking studies were performed that suggest that compounds 4a–e bind to cyclooxygenase (COX)-1 and COX-2 isoforms, but with higher affinity for COX-2. The compounds display similar anti-inflammatory activities in vivo, although compound 4c is the most effective compound for inhibiting rat paw edema, with a reduction in the extent of inflammation of 35.9% and 52.8% at 2 and 4 h, respectively. The anti-inflammatory activity of N-acyl hydrazone derivatives was inferior to their respective parent drugs, except for compound 4c after 5 h. Ulcerogenic studies revealed that compounds 4a–e are less gastrotoxic than the respective parent drug. Compounds 4b–e demonstrated mucosal damage comparable to celecoxib. The in vivo analgesic activities of the compounds are higher than the respective parent drug for compounds 4a–b and 4d–e. Compound 4a was more active than dipyrone in reducing acetic-acid-induced abdominal constrictions. Our results indicate that compounds 4a–e are anti-inflammatory and analgesic compounds with reduced gastrotoxicity compared to their respective parent non-steroidal anti-inflammatory drugs.

Evaluation and degradation chemistry of orbifloxacin using LC-MS

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Co-simulation tools for networked control systems: revision and utilization

Networked control systems (NCSs) are distributed control systems in which the sensors, actuators, and controllers are physically separated and connected through an industrial network. The main challenge related to the development of NCSs is the degenerative effects caused by the inclusion of this communication network in the closed loop control. In order to mitigate these effects, co-simulation tools for NCS have been developed to study the network influence in the NCS. This paper presents a revision about co-simulation tools for NCS and the application of two of these tools for the design and evaluation of NCSs. The TrueTime and Jitterbug tools were used together to evaluate the main configuration parameter that affects the performance of CAN-based NCS and to verify the NCS quality of control under various timing conditions including different transmission period of messages and network delays. Therefore, the simulation results led to the conclusion that despite the transmission period of messages is the most significant factor among the analyzed in the design of NCS, its influence is related to the kind of system with greater effects in NCSs with fast dynamics.

Evaluation of Electrical Resistivity in a Tropical Sandy Soil Compacted

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Genetic erosion risk by environmental and antropic factor applied on strategies for Lychnophora ericoides conservation

This study evaluated the genetic erosion risk factors and the strategic points for the conservation of Lychnophora ericoides population in “Paraíso Perdido” farm, Serra da Canastra (20° 37’ 54” S; 46° 19’ 37” W; 833 m height) in São João Batista do Glória City, Minas Gerais State, Brazil. The number of young and adult plants, the soil and the phenology were evaluated in two sample areas of 125 m2. Information about the species utilization was obtained with local informants. Data on the region were obtained through literature review, in loco evaluation, GPS and geo-referenced map. In addition, local use of the plant for mixtures of drug was evaluated. According to the results obtained, the soil of the population is lithic with a weathered portion of frank-sandy texture, very acidic and dystrophic. The population density is 0.16 individuals/m2, 0.078 young/adult plant. The predominant phenophase was fruiting (100% plants) followed by flowering (21.62% plants). The local community uses the leaves of the plant in the form of hydroalcoholic extracts, as anti-inflammatory. Based on the evaluated parameters, the population is at 73% risk of genetic erosion. The detected key points were the development of activities including the participation of the local community for habitat protection as well as germplasm collection, seedlings production and reintroduction, together with environmental education, supervision, and reduction in the propensity for fire.