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1.
J Synchrotron Radiat ; 23(1): 59-66, 2016 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-26698046

RESUMEN

Adjustable mirrors equipped with piezo actuators are commonly used at synchrotron and free-electron laser (FEL) beamlines, in order to optimize their focusing properties and sometimes to shape the intensity distribution of the focal spot with the desired profile. Unlike them, X-ray mirrors for astronomy are much thinner in order to enable nesting and reduce the areal mass, and the application of piezo actuators acting normally to the surface appears much more difficult. There remains the possibility to correct the deformations using thin patches that exert a tangential strain on the rear side of the mirror: some research groups are already at work on this approach. The technique reported here relies on actively integrating thin glass foils with commercial piezoceramic patches, fed by voltages driven by the feedback provided by X-rays, while the tension signals are carried by electrodes on the back of the mirror, obtained by photolithography. Finally, the shape detection and the consequent voltage signal to be provided to the piezoelectric array will be determined by X-ray illumination in an intra-focal setup at the XACT facility. In this work, the manufacturing steps for obtaining a first active mirror prototype are described.

2.
Artículo en Inglés | MEDLINE | ID: mdl-33207370

RESUMEN

Crystalline rocks can produce dangerous radiation levels on the basis of their content in radioisotopes. Here, we report radiological data from 10 metamorphic and igneous rock samples collected from the crystalline basement of the Peloritani Mountains (southern Italy). In order to evaluate the radiological properties of these rocks, the gamma radiation and the radon emanation have been measured. Moreover, since some of these rocks are employed as building materials, we assess the potential hazard for population connected to their use. Gamma spectroscopy was used to measure the 226Ra, 232Th and 40K activity concentration, whereas the radon emanation was investigated by using a RAD 7 detector. The results show 226Ra, 232Th and 40K activity concentration values ranging from (17 ± 4) to (56 ± 8) Bq kg-1, (14 ± 3) to (77 ± 14) Bq kg-1 and (167 ± 84) to (1760 ± 242) Bq kg-1, respectively. Values of the annual effective dose equivalent outdoor range from 0.035 to 0.152 mSv y-1, whereas the gamma index is in the range of 0.22-0.98. The 222Rn emanation coefficient and the 222Rn surface exhalation rate vary from (0.63 ± 0.3) to (8.27 ± 1.6)% and from (0.12 ± 0.03) to (2.75 ± 0.17) Bq m-2 h-1, respectively. The indoor radon derived from the building use of these rocks induces an approximate contribution to the annual effective dose ranging from 8 to 176 µSv y-1. All the obtained results suggest that the crystalline rocks from the Peloritani Mountains are not harmful for the residential population, even though they induce annual effective doses due to terrestrial gamma radiation above the worldwide average values. Moreover, their use as building materials does not produce significant health hazards connected to the indoor radon exposure.

3.
Tissue Cell ; 40(2): 89-94, 2008 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-18155116

RESUMEN

Since glucocorticoids have a role in maintaining the homeostatic status in fish, in the present paper mRNA expression (in situ hybridization) and tissue immunohistochemical localization of a glucocorticoid receptor (DlGR1) in several Dicentrarchus labrax organs are reported. Riboprobe and specific antibodies were prepared by using the DlGR1 that has been previously cloned and sequenced from peritoneal cavity leukocytes. Both mRNA and receptor were identified in head kidney, spleen, gills, intestine, heart and liver tissues. The functional roles of DlGR1 localization are discussed.


Asunto(s)
Lubina/metabolismo , Proteínas de Peces/metabolismo , Receptores de Glucocorticoides/metabolismo , Animales , Lubina/genética , Western Blotting , Proteínas de Peces/genética , Expresión Génica , Inmunohistoquímica , Hibridación in Situ , ARN Mensajero/análisis , Receptores de Glucocorticoides/genética
4.
Geobiology ; 15(5): 664-677, 2017 09.
Artículo en Inglés | MEDLINE | ID: mdl-28383164

RESUMEN

Ammonium- and Fe(II)-rich fluid flows, known from deep-sea hydrothermal systems, have been extensively studied in the last decades and are considered as sites with high microbial diversity and activity. Their shallow-submarine counterparts, despite their easier accessibility, have so far been under-investigated, and as a consequence, much less is known about microbial communities inhabiting these ecosystems. A field of shallow expulsion of hydrothermal fluids has been discovered at depths of 170-400 meters off the base of the Basiluzzo Islet (Aeolian Volcanic Archipelago, Southern Tyrrhenian Sea). This area consists predominantly of both actively diffusing and inactive 1-3 meters-high structures in the form of vertical pinnacles, steeples and mounds covered by a thick orange to brown crust deposits hosting rich benthic fauna. Integrated morphological, mineralogical, and geochemical analyses revealed that, above all, these crusts are formed by ferrihydrite-type Fe3+ oxyhydroxides. Two cruises in 2013 allowed us to monitor and sampled this novel ecosystem, certainly interesting in terms of shallow-water iron-rich site. The main objective of this work was to characterize the composition of extant communities of iron microbial mats in relation to the environmental setting and the observed patterns of macrofaunal colonization. We demonstrated that iron-rich deposits contain complex and stratified microbial communities with a high proportion of prokaryotes akin to ammonium- and iron-oxidizing chemoautotrophs, belonging to Thaumarchaeota, Nitrospira, and Zetaproteobacteria. Colonizers of iron-rich mounds, while composed of the common macrobenthic grazers, predators, filter-feeders, and tube-dwellers with no representatives of vent endemic fauna, differed from the surrounding populations. Thus, it is very likely that reduced electron donors (Fe2+ and NH4+ ) are important energy sources in supporting primary production in microbial mats, which form a habitat-specific trophic base of the whole Basiluzzo hydrothermal ecosystem, including macrobenthic fauna.


Asunto(s)
Compuestos de Amonio/metabolismo , Archaea/metabolismo , Bacterias/metabolismo , Ecosistema , Compuestos Ferrosos/metabolismo , Respiraderos Hidrotermales/microbiología , Hierro/metabolismo , Crecimiento Quimioautotrófico , Islas del Mediterráneo , Erupciones Volcánicas
5.
Artículo en Inglés | MEDLINE | ID: mdl-11041540

RESUMEN

1. Patch-clamp technique was used in primary cultures of cerebellar granule neurons to study the modulation of the cyclothiazide analogue (IDRA21) and of the diazoxide derivative (IDRA 5) on KA-evoked currents. 2. The dose-response of kainic acid (KA) reveals an EC50=90 microM and an Hill coefficient of 1.3. IDRA 21 and cyclothiazide potentiate KA-evoked current in a dose dependent way, being cyclothiazide more potent but less efficacious than IDRA 21. Conversely IDRA 5 acts as a negative modulator of KA evoked -current. 3. Application of IDRA 21 and cyclothiazide results in a current potentiation of 125+/-18% and 80+/-12% respectively, while IDRA 5 decreases KA-current (-21+/-5%). Coapplication of cyclothiazide and IDRA 21 produces a potentiation of 110+/-17%, suggesting a competition of the two drugs for the same site. 4. In the same experimental model we studied the ability of IDRA compounds of promoting toxicity through AMPA-receptor activation. Under basal conditions AMPA treatment (50 microM for 1 hour) results in a negligible excitotoxicity. 5. In contrast similar treatment with AMPA + IDRA 21 (1 mM) or + IDRA 5 (1 mM) or + cyclothiazide (100 microM) induces citotoxicity. The neurotoxic damage induced by IDRA 21 and cyclothiazide is blocked by GYKI 53655 (50 microM) and by NBQX (10 microM). Interestingly GYKI and NBQX are ineffective in reducing IDRA 5 toxicity.


Asunto(s)
Benzotiadiazinas/farmacología , Diazóxido/farmacología , Receptores de Glutamato/efectos de los fármacos , Vasodilatadores/farmacología , Potenciales de Acción/efectos de los fármacos , Potenciales de Acción/fisiología , Animales , Cerebelo/efectos de los fármacos , Cerebelo/fisiología , Electrofisiología , Ácido Kaínico/farmacología , Técnicas de Placa-Clamp , Ratas , Ratas Sprague-Dawley , Receptores de Glutamato/fisiología , Vasodilatadores/agonistas
6.
J Pharm Biomed Anal ; 23(1): 33-40, 2000 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-10898152

RESUMEN

The formation of inclusion complexes between beta-cyclodextrin with the two beta-blockers, atenolol and celiprolol, have been studied in the aqueous environment and in the solid state by nuclear magnetic resonance (NMR) spectroscopy, X-ray, differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) techniques. The magnitude of the chemical shifts of the interior and exterior beta-cyclodextrin protons in the presence of each beta-blocker indicated that these are included within the beta-cyclodextrin cavity. In aqueous solution they form 1:1 complexes. In the solid state the formation of the beta-cyclodextrin/atenolol (celiprolol) complexes is confirmed by X-ray, DSC and SEM, also employed to characterize pure substances and their physical mixtures.


Asunto(s)
Antagonistas Adrenérgicos beta/química , Rastreo Diferencial de Calorimetría , Espectroscopía de Resonancia Magnética , Microscopía Electrónica de Rastreo , Estructura Molecular , Difracción de Rayos X
7.
J Pharm Biomed Anal ; 20(1-2): 283-8, 1999 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-10704033

RESUMEN

The pseudo-first order rate constant for the hydrolysis of cinnoxicam as a function of temperature was obtained by variable-temperature kinetic experiments. The method used is on a generalization of non-isothermal analysis, and takes advantage of the capabilities of modern data collection and processing systems. A spectrophotometric method under non isothermal conditions was carried out. The results obtained are identical to those obtained under the same conditions by using traditional constant-temperature kinetic runs. This provides the possibility of reducing the amount of time spent and chemicals usually used in collecting kinetic data in mechanistic studies in solution by an order of magnitude.


Asunto(s)
Antiinflamatorios no Esteroideos/análisis , Piroxicam/análogos & derivados , Algoritmos , Cápsulas , Cromatografía Líquida de Alta Presión , Cromatografía en Capa Delgada , Estabilidad de Medicamentos , Hidrólisis , Cinética , Piroxicam/análisis , Soluciones , Temperatura
8.
J Pharm Biomed Anal ; 29(6): 1005-14, 2002 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-12110385

RESUMEN

Flavonoids are natural substances with a lot of biological activities, including the antioxidant one. Their use in pharmaceutical field is, however, limited by their aqueous insolubility. As the formation of the inclusion complexes can improve their solubility in water, the flavonoids hesperetin, hesperidin, naringenin and naringin have been complexed with beta-cyclodextrin (beta-CD) by the coprecipitation method and studied in solution and in solid state by NMR, FT-IR, differential scanning calorimetry and X-ray techniques. The effects of complexation on the chemical shifts of the internal and external protons of beta-CD in the presence of each flavonoid were observed.


Asunto(s)
Ciclodextrinas/análisis , Flavonoides/análisis , beta-Ciclodextrinas , Rastreo Diferencial de Calorimetría , Ciclodextrinas/química , Portadores de Fármacos/análisis , Portadores de Fármacos/química , Flavonoides/química , Espectroscopía de Resonancia Magnética , Solubilidad , Soluciones , Espectroscopía Infrarroja por Transformada de Fourier , Difracción de Rayos X
9.
Minerva Med ; 78(12): 815-22, 1987 Jun 30.
Artículo en Italiano | MEDLINE | ID: mdl-3601129

RESUMEN

Peripheral atherosclerotic arteriopathies are characterised by increased blood viscosity and, according to some, by a reduction in red blood cell deformability. Red blood cell viscosity was studied in 40 atherosclerosic patients (14 carotid and 26 aortoiliacofemoral lesions). All patients were subjected to the standard diagnostic examination (Doppler velocimetry, etc.). Fifty healthy non-smokers of the same sex and 20 heavy smokers were studied as controls. The viscosity of the whole blood, and plasma and blood fibrinogen were assayed. In studying erythrocyte viscosity, cells poor in leucocytes and platelets suspended in a saline phosphate buffer were employed. The atherosclerotic patients presented significantly higher mean levels of erythrocyte viscosity (p less than 0.01) and the increase in plasma viscosity and blood fibrinogen was also statistically significant. The viscosity of the whole blood was also increased in these patients (p less than 0.001). The increase in blood viscosity in subjects with peripheral arteriopathies therefore appears to be attributable to the plasma and to rheological alterations in the red blood cells.


Asunto(s)
Arteriosclerosis/sangre , Viscosidad Sanguínea , Deformación Eritrocítica , Adulto , Anciano , Femenino , Fibrinógeno/análisis , Hematócrito , Humanos , Masculino , Persona de Mediana Edad , Fumar
10.
Minerva Med ; 78(13): 893-8, 1987 Jul 15.
Artículo en Italiano | MEDLINE | ID: mdl-3601134

RESUMEN

Cigarette smoking, hypercholesterolaemia, hypertriglyceridaemia, are all known risk factors for atherosclerotic vascular lesions. Often they are associated with alterations mainly due to increased haematocrit (smoking) or to the influence of triglycerides and cholesterol on the erythrocyte membrane or plasma viscosity. In order to eliminate these factors, washed red blood cells, poor in leucocytes and platelets, in a suspension with phosphate saline buffer were studied. 20 heavy smokers, 40 patients with hyperlipidaemia (26 II a or b; 14 IV) and 50 healthy people were considered. Red blood cell viscosity was calculated at 4 shear rate between 0.37 and 69.5 sec-1. Red blood cell deformability, as an indicator of cell filtration through Nucleopore membranes was also studied. There was no difference in the filtration index among the subjects under study. Red blood cell viscosity increased in smokers and in patients with hyperlipidaemia.


Asunto(s)
Viscosidad Sanguínea , Deformación Eritrocítica , Hiperlipidemias/sangre , Fumar , Adulto , Arteriosclerosis/etiología , Femenino , Hematócrito , Humanos , Masculino , Persona de Mediana Edad , Reología , Riesgo
11.
Minerva Med ; 78(13): 899-906, 1987 Jul 15.
Artículo en Italiano | MEDLINE | ID: mdl-3601135

RESUMEN

Risk factors for atherosclerosis are often associated with haemorheological changes. On this point, obesity (recently advocated as an independent risk factor) was not much studied and with not univocal results. We have studied 70 obese patients (BMI greater than 30) and 50 healthy subjects (BMI less than 25). Among obese 26 had no more pathologies, 29 had hypertension, 3 suffered from ischemic heart disease, 3 suffered from occlusive arteriopathy, 9 were hyperlipidemic, 10 were smokers. We determined plasma viscosity and whole blood viscosity (at haematocrit corrected to 45% too). Washed erythrocytes, poor in leucocytes and platelets and resuspended in phosphate-buffered saline, were used for study of erythrocyte viscosity and deformability. Obese patients showed raised mean blood viscosity values when compared to healthy controls (p less than 0.01); an even more significant increase (p less than 0.001) was found concerning plasma viscosity and fibrinogen. Erythrocyte viscosity and red blood cell filterability index did not show any significant difference. We found no significant correlation between viscosity values and presence of hypertension, hyperlipidemia and smoking habit among obese. In conclusion, the higher vasculopathy incidence might be caused by an increase in blood viscosity, mostly due to plasmatic component. This fact appears to be independent from the presence of atherosclerosis complications or other risk factors.


Asunto(s)
Viscosidad Sanguínea , Deformación Eritrocítica , Hematócrito , Obesidad/sangre , Adulto , Anciano , Femenino , Fibrinógeno/análisis , Humanos , Masculino , Persona de Mediana Edad , Reología
12.
Farmaco ; 44(12): 1129-40, 1989 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-2517471

RESUMEN

The 1-octanol/water partition coefficients of a series of antimicrobial S-aryl(tetramethyl)isothiouronium salts, were determined. The concentration of the solute in the two phases was measured by means of HPLC. The values of the hydrophobic parameters thus obtained were correlated to the corresponding capacity factors (log Kw) and compared with those expected on the basis of additive-constitutive principles. The deviations were interpreted quantitatively on the basis of electronic interactions of the substituents in the benzene ring. Equations correlating structural features and antimicrobial activity of some studied compounds by means of molecular parameters were formulated.


Asunto(s)
Antibacterianos/síntesis química , Isotiuronio/análogos & derivados , Tiourea/análogos & derivados , Bacterias/efectos de los fármacos , Fenómenos Químicos , Química , Química Física , Cromatografía Líquida de Alta Presión , Isotiuronio/síntesis química , Isotiuronio/farmacología , Pruebas de Sensibilidad Microbiana , Staphylococcus aureus/efectos de los fármacos , Streptococcus pyogenes/efectos de los fármacos
13.
Farmaco ; 45(6): 631-45, 1990 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-2176787

RESUMEN

In this study we tested the potential taurine-antagonistic properties of three rigid analogs of taurine, 3-amino- (1), 3-hydrazino- (2) and 3-aminomethyl-1,2,4-benzothiadiazine-1,1-dioxide (3), which were prepared in our laboratory, using TAG (6-aminomethyl-3-methyl-1,2,4-benzothiadiazine-1,1- dioxide) (4), the only antagonist of taurine so far available, as reference compound in "in vivo" and "in vitro" experiments. Some physicochemical properties of (1), (2) and (3) were studied and the synthesis of TAG (4) was improved with a new preparative method. A dose-effect study performed by injecting intracerebroventricularly (1), (2) and (3) showed that these compounds have none of exciting effects exerted by the high doses of TAG (4). (1) and (3) as well as TAG (4), were found to antagonize the controlateral turning induced by the intracerebro injection of taurine and to potentiate the sedative effect of diazepam. We failed to find specific binding for taurine in different brain synaptic membrane preparations using 3H-taurine as radioligand and taurine, (1) and (3) as binding displacer. (1), (3) and TAG (4) however were found to antagonize the inhibitory effect of taurine on 3H-diazepam binding. These results seem to indicative that at least (1) and (3), which were more extensively studied than (2) because of their better solubility, are taurine antagonists with an apparent better selectivity than TAG (4).


Asunto(s)
Taurina/análogos & derivados , Taurina/antagonistas & inhibidores , Animales , Conducta Animal/efectos de los fármacos , Unión Competitiva/efectos de los fármacos , Fenómenos Químicos , Química , Diazepam/metabolismo , Relación Dosis-Respuesta a Droga , Técnicas In Vitro , Inyecciones Intraventriculares , Masculino , Ratas , Ratas Endogámicas , Receptores de GABA-A/efectos de los fármacos , Receptores de GABA-A/metabolismo , Membranas Sinápticas/efectos de los fármacos , Membranas Sinápticas/metabolismo , Taurina/metabolismo
14.
Farmaco ; 45(6): 617-30, 1990 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-2148672

RESUMEN

A series of carbamimidothioic acid phenylmethyl ester salts and their N,N'-tetramethyl derivatives were synthesized, many of which exert an interesting inhibiting action on Gram-positive and Gram-negative bacteria and also on fungi. This activity is noteworthy in view of the large number of strains antagonized; the (3,4,5-trichlorophenyl) methyl ester chloride of carbamimidothioic acid appeared to be the best term of the series. The possible influence on this activity of decomposition kinetics to the corresponding mercapto-derivatives was investigated and compared with that of a series of N,N'-tetramethyl derivatives of previously studied carbamimidothioic acid phenyl ester salts.


Asunto(s)
Antiinfecciosos/síntesis química , Tiourea/síntesis química , Antibacterianos , Antiinfecciosos/análisis , Bacterias/efectos de los fármacos , Fenómenos Químicos , Química , Hongos/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Cinética , Pruebas de Sensibilidad Microbiana , Espectrofotometría Ultravioleta , Tiourea/análisis , Tiourea/farmacología
15.
Farmaco ; 48(10): 1463-73, 1993 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-8117384

RESUMEN

The influence of 11 newly synthesized 2,6-bis(1,1-dimethylethyl)phenol derivatives substituted in the 4 position as measured on the carrageenan paw edema assay in Sprague-Dawley rats, was studied using indomethacin as a reference drug. Furthermore we studied the possible interference of few of these compounds on the calcium binding sites by using the specific ligand [3H]-PN 200-110 in "in vitro" experiments. As far as regard the antiinflammatory activity only the compounds 2b, 2j and 2k, dosed at 20 mg/Kg/os, exerted an inhibitory effect on paw edema which was practically equal, after 6 h, to that of indomethacin (approximately 30%) dosed at 2.5 mg/Kg. The compound 2k, however, showed, in comparison with indomethacin and the other new tested compounds, a longer lasting effect, reaching, after 8 h, a 56.7% inhibition of the edema. Finally the above mentioned compounds, when tested alone or in combination with nitrendipine, did not exert any displacing activity on [3H]-PN 200-110 binding to synaptosomal membranes. It is noteworthy however that compound 2e, which incidentally was inactive as antiinflammatory agent, showed a negative allosteric modulatory activity on the ability of nitrendipine to displace [3H]-PN 200-110 binding.


Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Antiinflamatorios no Esteroideos/farmacología , Fenoles/síntesis química , Fenoles/farmacología , Animales , Sitios de Unión/efectos de los fármacos , Calcio/química , Carragenina , Edema/inducido químicamente , Edema/prevención & control , Femenino , Isradipino/metabolismo , Masculino , Nitrendipino/farmacología , Ratas , Ratas Sprague-Dawley , Sinaptosomas/química , Sinaptosomas/efectos de los fármacos
16.
Pharmazie ; 45(9): 680-1, 1990 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-2284312

RESUMEN

The scavenging activity of some isosteric antiinflammatory heteoarylalkanoic acids with respect to oxygen-free radicals has been studied. All the compounds were found to inhibit the depolymerization of hyaluronic acid due to enzymatically or chemically generated hydroxyl radicals. The reduced consumption of oxygen by xanthine oxidase indicates a cotemporaneous phenomenon of enzymatic inhibition.


Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Ácidos Carboxílicos/síntesis química , Óxidos S-Cíclicos/síntesis química , Depuradores de Radicales Libres , Ácidos Carboxílicos/farmacología , Óxidos S-Cíclicos/farmacología , Consumo de Oxígeno/efectos de los fármacos , Xantina Oxidasa/metabolismo
17.
Pharmazie ; 43(1): 37-9, 1988 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-3375300

RESUMEN

A series of dialkylamino, pyrrolidyl and morpholyl-alkyl-derivatives of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide, 7- or 5,7-halogen substituted in the benzenoid moiety, was prepared and their cardiovascular activity studied. Most of the substances in question were capable of inducing a significant decrease in mean arterial blood pressure; some of them tended to increase pulse pressure or to cause bradycardia, an effect which was noted particularly in the case of compound 10 which reduced heart-rate by 85%. The structure/activity relationship of these substances, of the 6- and 6,7-halogen substituted isomers and of their corresponding non-substituted progenitors is examined.


Asunto(s)
Benzotiadiazinas/síntesis química , Fármacos Cardiovasculares/síntesis química , Animales , Benzotiadiazinas/farmacología , Presión Sanguínea/efectos de los fármacos , Fármacos Cardiovasculares/farmacología , Fenómenos Químicos , Química , Óxidos S-Cíclicos/síntesis química , Óxidos S-Cíclicos/farmacología , Electrocardiografía , Frecuencia Cardíaca/efectos de los fármacos , Hemodinámica/efectos de los fármacos , Masculino , Ratas , Ratas Endogámicas , Estereoisomerismo
18.
Pharmazie ; 44(9): 601-4, 1989 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-2608704

RESUMEN

A series of 3-(4H-1,2,4-benzothiadiazine-1,1-dioxide-3-yl-thio)-propanoic acids was synthesized in order to study their possible antiinflammatory in comparison with the corresponding lower homologues and isosters previously studied. Most of the compounds proved effective against carrageenan-induced plantar oedema. The possible influence of some chemico-physical parameters on the occurrence of this biological activity was investigated.


Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Benzotiadiazinas/síntesis química , Óxidos N-Cíclicos/síntesis química , Propionatos/síntesis química , Animales , Antiinflamatorios no Esteroideos/farmacología , Benzotiadiazinas/farmacología , Fenómenos Químicos , Química Física , Óxidos N-Cíclicos/farmacología , Masculino , Propionatos/farmacología , Ratas , Ratas Endogámicas
19.
Boll Chim Farm ; 129(7-8): 248-50, 1990.
Artículo en Inglés | MEDLINE | ID: mdl-2095810

RESUMEN

The rates of reaction toward cysteine of a series of carbamimidothioic acid phenylmethylesters halides were investigated in phosphate buffer pH 7.4 at 37 degrees C under pseudo-first-order conditions. The reaction involves nucleophilic attack of cysteine on the C-S bond of isothiouronium mojety and corresponding benzenemethanethiols were detected as product of the reaction. Apparent first-order rate constants were determined.


Asunto(s)
Antiinfecciosos/química , Cisteína/química , Tiocarbamatos/química , Tiocarbamatos/farmacología
20.
Boll Chim Farm ; 129(9): 273-5, 1990 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-2098054

RESUMEN

The antitumor activity of the methyl-6-chloro-4H-1,2,4-benzothiadiazin-3-yl-S-carbamothioate+ ++-S,S,-dioxide (1) and the methyl-4H-1,2,4-benzothiadiazin-3-yl-carbamodithioate-S,S-di oxide (2), has been evaluated. Compound 2 passed activity criteria for leukemia P388 and was also moderately active against transplanted mouse tumor L1210 leukemia and M5076 sarcoma.


Asunto(s)
Antineoplásicos/farmacología , Tiadiazinas/farmacología , Tiocarbamatos/farmacología , Animales , Humanos , Ratones , Ratones Endogámicos , Neoplasias Experimentales/tratamiento farmacológico
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