3D geophysical imaging for site-specific characterization plan of an old landfill.

As it is well-known, the characterization plan of an old landfill site is the first stage of the project for the treatment and reclamation of contaminated lands. It is a preliminary in-situ study, with collection of data related to pollution phenomena, and is aimed at defining the physical properties and the geometry of fill materials as well as the possible migration paths of pollutants to the surrounding environmental targets (subsoil and groundwater). To properly evaluate the extent and potential for subsoil contamination, waste volume and possible leachate emissions from the landfill have to be assessed. In such perspective, the integrated use of geophysical methods is an important tool as it allows a detailed 3D representation of the whole system, i.e. waste body and hosting environment (surrounding rocks). This paper presents a very accurate physical and structural characterization of an old landfill and encasing rocks obtained by an integrated analysis of data coming from a multi-methodological geophysical exploration. Moreover, drillings were carried out for waste sampling and characterization of the landfill body, as well as for calibration of the geophysical modeling.

A low tilt waveform in the transthoracic defibrillation of ventricular arrhythmias during cardiac arrest.

AIM: Most commercially available defibrillators utilise a high tilt waveform. Work in atrial fibrillation has shown improved defibrillation success using low tilt waveforms. We hypothesise that a novel low tilt biphasic waveform will be non-inferior to a standard tilt waveform whilst delivering lower energy for the defibrillation of ventricular arrhythmias. METHODS: Patients in cardiac arrest who experienced ventricular arrhythmias received shocks from a novel low tilt waveform defibrillator at 120J or a standard tilt waveform defibrillator at 150J. Resuscitation guidelines were followed as per Resuscitation Council UK, 2005. A shock was successful when the ventricular arrhythmia was terminated for ≥ 5s following shock delivery. RESULTS: A total of 113 cardiac arrest cases were included. The low tilt device was used for 56 cases and the standard tilt device for 57 cases. The presenting rhythm was ventricular fibrillation (VF) in 71.7% (81/113), pulseless electrical activity (PEA) in 15.9% (18/113), ventricular tachycardia (VT) in 9.7% (11/113), asystole in 1.8% (2/113) and narrow complex rhythm in 0.9% (1/113). The low tilt device resulted in first shock success in 86% (48/56 cases) vs. the standard tilt device first shock success of 77% (44/57 cases). There was no significant difference in first shock success between the two devices (p=0.36). CONCLUSION: The low tilt waveform used in this study demonstrated first shock success rates in keeping with a commercially available high tilt defibrillator which could result in less myocardial damage due to reduced energy requirements.

Finite driving rate and anisotropy effects in landslide modeling.

In order to characterize landslide frequency-size distributions and individuate hazard scenarios and their possible precursors, we investigate a cellular automaton where the effects of a finite driving rate and the anisotropy are taken into account. The model is able to reproduce observed features of landslide events, such as power-law distributions, as experimentally reported. We analyze the key role of the driving rate and show that, as it is increased, a crossover from power-law to non-power-law behaviors occurs. Finally, a systematic investigation of the model on varying its anisotropy factors is performed and the full diagram of its dynamical behaviors is presented.

New thiadiazine derivatives with activity against Trypanosoma cruzi amastigotes.

The cytotoxicity of 18 new 1,2,6-thiadiazin-3,5-dione 1,1-dioxides was evaluated. This group of products was previously assayed against epimastigotes of Trypanosoma cruzi and some of them showed a high antiprotozoal activity. Thereafter 13 compounds with a high anti-epimastigote activity and low cytotoxicity were selected to be assayed against amastigotes. Some of the products showed the same or even lower cytotoxicity than nifurtimox and benznidazole, but most of them were very toxic for macrophages at 100 microg/ml. Only one of the compounds had an anti-amastigote activity similar to that of reference drugs at 10 microg/ml, but unfortunately this disappeared at lower concentrations.

Synthesis and herbicidal activity of N-oxide derivatives.

As part of an ongoing program on the chemistry and biological activity of N-oxide-containing molecules, a number of novel 1,2, 5-oxadiazole N-oxide, benzo[1,2-c]1,2,5-oxadiazole N-oxide, and quinoxaline N,N'-dioxide derivatives were synthesized and evaluated for their herbicidal activity. Many of these compounds exhibited moderate to good herbicidal pre-emergence activity against Triticum aestivum. Dose-response studies were done on the more representative compounds (12, 20, and 26). The most active compound, butylcarbamoylbenzo[1,2-c]1,2,5-oxadiazole N-oxide, 26, displayed herbicidal activity at concentrations as low as 24 g/ha.

Synthesis and antitrypanosomal evaluation of E-isomers of 5-nitro-2-furaldehyde and 5-nitrothiophene-2-carboxaldehyde semicarbazone derivatives. structure-activity relationships.

Several novel semicarbazone derivatives were prepared from 5-nitro-2-furaldehyde or 5-nitrothiophene-2-carboxaldehyde and semicarbazides bearing a spermidine-mimetic moiety. All derivatives presented the E-configuration, as determined by NMR-NOE experiments. These compounds were tested in vitro as potential antitrypanosomal agents, and some of them, together with the parent compounds, 5-nitro-2-furaldehyde and 5-nitrothiophene-2-carboxaldehyde semicarbazone derivatives, were also evaluated in vivo using infected mice. Structure-activity relationship studies were carried out using voltammetric response and lipophilic-hydrophilic balance as parameters. Two of the compounds (1 and 3) displayed the highest in vivo activity. A correlation was found between lipophilic-hydrophilic properties and trypanocidal activity, high R(M) values being associated with low in vivo effects.

Neurotransmitters adenosine triphosphate and noradrenaline induce nitric oxide release in rat vas deferens.

1. In rat vas deferens, electrical field stimulation (EFS) evoked a muscular biphasic tetrodotoxin (TTX)-sensitive contractile response. 2. The amplitude of this response increased with the frequency of stimulation. 3. After each stimulation, nitric oxide (NO) release was assayed and found to be released in a frequency-dependent manner. 4. NO release also occurred after treatment with exogenous neurotransmitters, adenosine 5'-triphosphate (ATP) and noradrenaline (NA). 5. Prazosin and pyridoxalphosphate-6-azophenyl-2',4'-disulphonic acid (PPADS), respective antagonists of alpha1-adrenoceptors and P2x purinoceptors, inhibited NO release induced by NA and ATP. Both prazosin and PPADS inhibited NO release by EFS. 6. TTX failed to modify the NO release induced by exogenous neurotransmitters but abolished the release of NO and contractile response by EFS. 7. EFS and released noradrenaline and ATP induce the release of NO through postjunctional alpha1 -adrenoceptors and P2x-purinoceptors, respectively.

Synthesis and antichagasic properties of new 1,2,6-thiadiazin-3,5-dione 1,1-dioxides and related compounds.

In a search for antichagasic drugs, 14 new 4-(nitroarylidene)-1,2,6-thiadiazin-3,5-dione 1,1-dioxide derivatives were synthesized and tested in vitro against the epimastigote form of Trypanosoma cruzi and some of them showed important antiprotozoan activity. Attempts to synthesize new 4-(nitroarylidene)-3,5-diamino-1,2,6-thiadiazine 1,1-dioxides were unsuccessful. The antichagasic properties of nitroarylidene-malononitrile and nitroarylidene-cyanoacetamide derivatives, thus obtained, were also tested. The cytotoxic properties against Vero cells of compounds which showed remarkable in vitro antichagasic activity were evaluated. All compounds tested exhibited high toxicity percentages at 100 micrograms/ml. However, compound 3c showed in vitro antichagasic and cytotoxic properties such as nifurtimox at the dose of 10 micrograms/ml.

1,2,5-Oxadiazole N-oxide derivatives and related compounds as potential antitrypanosomal drugs: structure-activity relationships.

The syntheses of a new series of derivatives of 1,2,5-oxadiazole N-oxide, benzo[1,2-c]1,2,5-oxadiazole N-oxide, and quinoxaline di-N-oxide are described. In vitro antitrypanosomal activity of these compounds was tested against epimastigote forms of Trypanosoma cruzi. For the most effective drugs, derivatives IIIe and IIIf, the 50% inhibitory dose (ID50) was determined as well as their cytotoxicity against mammalian fibroblasts. Electrochemical studies and ESR spectroscopy show that the highest activities observed are associated with the facile monoelectronation of the N-oxide moiety. Lipophilic-hydrophilic balance of the compounds could also play an important role in their effectiveness as antichagasic drugs.

Nematocide activity of 6,7-diarylpteridines in three experimental models.

The in vitro nematocide activity of seventeen 6,7-diarylpteridines has been tested using three different experimental models, Caenorhabditis elegans, Nippostrongylus brasiliensis and Heligmosomoides polygyrus. The method of evaluation of inhibition in the secretion of acetylcholinesterase by H. polygyrus seems to be the most indicated to avoid false positives. The in vivo activities, against Trichinella spiralis, of the most in vitro active pteridines have been assayed. All pteridine derivatives bearing 6,7-di-p-bromophenyl substituents have shown in vitro nematocide activities in the three experimental models used. Amongst all the pteridines tested in vivo, only 2,4-pteridinedithione derivatives exhibited moderate activity.

Synthesis and biological evaluation of 1,2,5-oxadiazole N-oxide derivatives as hypoxia-selective cytotoxins.

Synthesis and biological evaluation of new 1,2,5-oxadiazole N-oxide derivatives with potential cytotoxic effects are described. From the series of compounds tested, compounds 2 and 6 proved to be very active, although non-selective.

Synthesis and anti-trypanosomal activity of novel 5-nitro-2-furaldehyde and 5-nitrothiophene-2-carboxaldehyde semicarbazone derivatives.

Several novel semicarbazones derivatives were prepared from 5-nitro-2-furaldehyde or 5-nitrothiophene-2-carboxaldehyde, and tested in vitro as potential anti-trypanosomal agents. The compounds were prepared in good to excellent yields in 2-3 steps from readily available starting materials. Some derivatives were found to be active against Trypanosoma cruzi with an activity similar to that of Nifurtimox.