Novel 1,3,5-Triazinyl Aminobenzenesulfonamides Incorporating Aminoalcohol,Aminochalcone and Aminostilbene Structural Motifs as Potent Anti-VRE Agents,and Carbonic Anhydrases I,II, VII,IX, and XII Inhibitors

A series of 1,3,5-triazinyl aminobenzenesulfonamides substituted by aminoalcohol, aminostilbene, and aminochalcone structural motifs was synthesized as potential human carbonic anhydrase (hCA) inhibitors. The compounds were evaluated on their inhibition of tumor-associated hCA IX and hCA XII, hCA VII isoenzyme present in the brain, and physiologically important hCA I and hCA II. While the test compounds had only a negligible effect on physiologically important isoenzymes, many of the studied compounds significantly affected the hCA IX isoenzyme. Several compounds showed activity against hCA XII; (E)-4-{2-[(4-[(2,3-dihydroxypropyl)amino]-6-[(4-styrylphenyl)amino]-1,3,5-triazin-2-yl)amino]ethyl}benzenesulfonamide (31) and (E)-4-{2-[(4-[(4-hydroxyphenyl)amino]-6-[(4-styrylphenyl)amino]-1,3,5-triazin-2-yl)amino]ethyl}benzenesulfonamide (32) were the most effective inhibitors with K_Is = 4.4 and 5.9 nM, respectively. In addition, the compounds were tested against vancomycin-resistant Enterococcus faecalis (VRE) isolates. (E)-4-[2-({4-[(4-cinnamoylphenyl)amino]-6-[(4-hydroxyphenyl)amino]-1,3,5-triazin-2-yl}amino)ethyl]benzenesulfonamide (21) (MIC = 26.33 µM) and derivative 32 (MIC range 13.80–55.20 µM) demonstrated the highest activity against all tested strains. The most active compounds were evaluated for their cytotoxicity against the Human Colorectal Tumor Cell Line (HCT116 p53 +/+). Only 4,4’-[(6-chloro-1,3,5-triazin-2,4-diyl)bis(iminomethylene)]dibenzenesulfonamide (7) and compound 32 demonstrated an IC₅₀ of ca. 6.5 μM; otherwise, the other selected derivatives did not show toxicity at concentrations up to 50 µM. The molecular modeling and docking of active compounds into various hCA isoenzymes, including bacterial carbonic anhydrase, specifically α-CA present in VRE, was performed to try to outline a possible mechanism of selective anti-VRE activity.     

Test run of biodiesel in public transport system in Belgrade

The problems related to our strong dependency on fossil fuels, i.e. greenhouse effect, energy dependency, urban pollution, are of growing importance in recent years. European Union (EU) Action plan of 2003, which had originated from Kyoto Agreement, defined a strategy for substitution of 20% of conventional fuel with the alternative one by 2020. Proved advantages of biodiesel usage in the system of public transport of passengers, with regard to exhaust gases emission above all, have been the decisive determinants for the actual promotion of biodiesel as ecologically “clean” fuel, while its wider usage gives important contribution to sustainable development of cities. This paper presents results of biodiesel-test run in Belgrade, as a part of the project BIO-PEX, which relates to the usage of this alternative fuel in real operating conditions in urban public transport system, with special emphasis on technical, ecological and operational aspects of biofuel usage.     

A chiral conjugated oligomer based on 1,1′-binaphthol with 3,3′-acetylene spacer

Summary. A 1,1'-binaphthol based optically active oligomer 6 with 3,3'-acetylene spacer was prepared from 2,2'-dimethoxy-1,1'-binaphthalene 3 through the palladium-catalyzed Stille coupling reaction. The high optical rotation and CD spectrum varified the main chain chirality of the oligomer. The photophysical properties of 6, absorption, excitation and fluorescent spectra, demonstrated that the oligomer molecule had a conjugated structure, but twisting and rigid conformation would reduce the delocalization along the backbone.     

Mood and symptom reporting among middle-aged women: The relationship between menopausal status, hormone replacement therapy, and exercise participation.

Vasomotor, somatic, and psychological symptoms associated with menopause are often treated with hormone replacement therapy (HRT), but the role of nonpharmacological interventions has received little attention. Two studies used the Profile of Mood States (POMS) and Women's Health Questionnaire (WHQ) to examine the effects of exercise among 4 groups of Australian women: premenopausal, perimenopausal, postmenopausal without HRT, and postmenopausal with HRT. Study 1, a comparison of exercisers and nonexercisers, showed that exercisers' moods were significantly more positive than sedentary women's moods, regardless of menopausal state. Exercising women also scored lower on somatic symptoms and memory-concentration difficulties. Study 2 examined the acute effects of aerobic exercise (premenopausal, postmenopausal without HRT, and postmenopausal with HRT) and found significant enhancements in mood and reductions in reported somatic and vasomotor symptoms immediately following an aerobic class. Exercise may assist in the alleviation of some menopausal symptoms. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Lycopene-rich cream obtained via high-pressure homogenisation of tomato processing residues in a water–oil mixture

Tomato processing residues are still rich in bioactive compounds that may be recovered and reused, with environmental and economic benefits. This short communication discloses for the first time that the high-pressure homogenisation (HPH) treatment of tomato residues in the presence of water and sunflower oil is able to promote the extraction of bioactive compounds concurrently to the formation of an oil-in-water emulsion stabilised by the micronized residues. The mechanical disruption effect of HPH improved the mass transfer of lycopene into the oil phase, and formed fine fibrous debris, improving stabilisation and visual appearance of the emulsion. Results showed a progressive increase of lycopene concentration in the cream phase up to 5 HPH passes and a concurrent reduction of its content in the pellet. Total polyphenols content and antioxidant activity in the aqueous phase gradually decreased when increasing the number of passes, suggesting their progressive transfer in the cream phase. The proposed process that relies on a purely physical treatment and uses only water/sunflower oil as extraction media resulted in the production of a lycopene-rich cream of potential use as a functional food ingredient.     

Encapsulation of Synthesized Plant Growth Regulator Based on Copper(II) Complex in Chitosan/Alginate Microcapsules

A new copper complex, trans-diaqua-trans-bis [1-hydroxy-1,2-di (methoxycarbonyl) ethenato] copper (abbreviation Cu(II) complex), was synthesized and its plant growth regulation properties were investigated. The results show a sharp dependence of growth regulation activity of the Cu(II) complex on the type of culture and its concentration. New plant growth regulator accelerated the development of the corn root system (the increase in both length and weight) but showed a smaller effect on the development of the wheat and barley root systems. Stimulation of corn growth decreased with increasing Cu(II) complex concentration from 0.0001% to 0.01% (inhibition at high concentrations—0.01%). The development of corn stems was also accelerated but to a lesser extent. Chitosan-coated calcium alginate microcapsules suitable for delivery of Cu(II) complex to plants were prepared and characterized. Analysis of the FTIR spectrum showed that complex molecular interactions between functional groups of microcapsule constituents include mainly electrostatic interactions and hydrogen bonds. Microcapsules surface exhibits a soft granular surface structure with substructures consisting of abundant smaller particles with reduced surface roughness. Release profile analysis showed Fickian diffusion is the rate-controlling mechanism of Cu(II) complex releasing. The obtained results give new insights into the complexity of the interaction between the Cu(II) complex and microcapsule formulation constituents, which can be of great help in accelerating product development for the application in agriculture     

The use of high stimulus rate auditory brainstem responses in the estimation of hearing threshold

Steady-state kinetics on the reaction catalyzed by the beta-glucosidase of Aspergillus niger were carried out to evaluate the kinetic parameters, Km and ko, for phenyl beta-D-glucosides. The ko/Km values, which may relate to productive binding at subsites, were found to correlate with the substituent constant pi (hydrophobicity), suggesting that subsite 2 has a hydrophobic character. A "hydrophobic-driven" mechanism is considered to contribute to the productive E-S complex for recognition of the substrate.     

Graphene synthesis by ion implantation

We demonstrate an ion implantation method for large-scale synthesis of high quality graphene films with controllable thickness. Thermally annealing polycrystalline nickel substrates that have been ion implanted with carbon atoms results in the surface growth of graphene films whose average thickness is controlled by implantation dose. The graphene film quality, as probed with Raman and electrical measurements, is comparable to previously reported synthesis methods. The implantation synthesis method can be generalized to a variety of metallic substrates and growth temperatures, since it does not require a decomposition of chemical precursors or a solvation of carbon into the substrate.     

Intestinal sleeve anastomosis: a comparative study with end-to-end anastomosis

This study examines the utility of a sleeve anastomosis with comparison to conventional end to end anastomosis. Thirty New Zealand white rabbits were randomized to sleeve (n = 15) or end-to-end (n = 15) small bowel anastomosis. Five rabbits of each group were sacrificed at 3 days, 7 days, and 6 weeks. Anastomoses were assessed for integrity, bursting strength, and stenosis and examined histologically. Ten control specimens of small bowel were tested for bursting pressure. Three rabbits died postoperatively (1 sleeve and 2 end-to-end). A fourth rabbit (sleeve) was sacrificed early at 3 weeks and had a total stenosis at the anastomosis. The remaining 26 rabbits were reoperated at the prescribed times. There was no evidence of infection or dehiscence in any of these rabbits. Both end-to-end and sleeve anastomoses were equivalent for bursting pressure at all times and, at 7 days and 6 weeks, were similar to controls. The stenotic index revealed no evidence of proximal dilation suggestive of obstruction in the 26 rabbits. For sleeve anastomoses the length of the projected bowel into the lumen persisted at the 6-week stage. Histologically there was good evidence of healing in both the sleeve and end-to-end anstomoses and the serosal surface of the sleeved bowel had epithelialized. Sleeve anastomosis has been demonstrated to heal well and to be as strong as conventional end-to-end anastomosis. Further studies are warranted to determine its role in intestinal anastomosis and potential as a valve.     

Grandparents and child passenger safety

Purpose

This study compares child passenger safety (CPS) practices of grandparents versus parents and determines grandparents’ opinions on car safety seats (CSS), barriers to use, and ways to transport grandchildren safely.

Methods

Observational surveys were conducted on a convenience sample of drivers transporting children younger than sixteen years at 25 locations by certified child passenger safety technicians observing children in motor vehicles and recorded use of child passenger restraints. The drivers were surveyed on their knowledge, attitudes, beliefs, and practices regarding CPS. Data from drivers identifying themselves as grandparents were analyzed; also, three grandparent focus groups provided opinions on CPS practices.

Results

During the study 1758 parents transporting 2713 children and 284 grandparents transporting 391 grandchildren were included. While most drivers were restrained and used child occupant restraints, almost 25% of parents and grandparents chose the incorrect seat to transport the child, and greater than 68% had at least one harness error. Grandparents were more likely to have looser lower anchor straps or seat belts and have children younger than thirteen years in the front seat.The focus group-grandparents had a favorable attitude toward CSS. Grandparents acknowledged the need for CSS but opined that CSS were difficult to use. Physical barriers included arthritis, back pain, mobility, decreased strength, and vision problems.

Conclusions

Grandparents and parents were equally likely to use CSS and choose correct seats. Compared to parents, grandparents were more likely to travel with their grandchildren with CSS installed with looser harnesses or an installed CSS with looser seat belt or lower anchors. Additionally, grandparents were more likely to have a child younger than thirteen years in the front seat. The use of community resources such as permanent fitting stations could help grandparents improve a grandchild's travel safety.