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Biomedical subjects

F Bruni

Publications and source records attributed to F Bruni.

At least 55 records · Page 3Linked to original sources
PubMed1991

Pharmacokinetics and pharmacodynamics of slow-release theophylline during treatment with nimesulide.

The pharmacodynamic and pharmacokinetic interactions were studied between nimesulide, a recently introduced non-steroidal anti-inflammatory drug, and theophylline, another highly protein-bound drug, in patients who were receiving slow-release theophylline for a chronic airflow-obstruction and who also needed anti-inflammatory treatment. A good tolerability was demonstrated of the two drugs association and there was an absence of pharmacodynamic interaction, as shown by lung function parameters, assayed before and after the coinciding nimesulide association. The pharmacokinetics of nimesulide and 4-hydroxy-nimesulide (its active metabolite) were not modified, in agreement with data shown by other authors. On the contrary, there was a slight alteration of theophylline pharmacokinetics, yet neither clinically nor biologically significant, probably due to an enzymatic induction.

Adolescent↗
PubMed1991

Clinical study on pharmacological interaction between nimesulide and warfarin.

This article describes the pharmacological interaction between nimesulide, a recently introduced non-steroidal anti-inflammatory drug, and warfarin, an indirect anticoagulant. The aim of the study was to demonstrate if nimesulide could potentiate the activity of this anticoagulant drug, as previously shown by some authors. Ten patients, who were taking 5 mg/day of warfarin, were treated with nimesulide 100 mg twice a day, for seven days: the association of the two drugs did not alter, in a statistical way, neither prothrombin time, nor partial thromboplastin time, nor fibrinogenemia, nor bleeding time. The findings showed that, in a short-term treatment, there was no bleeding risk in combining warfarin with nimesulide.

Adolescent↗
PubMed1991

Effect of cefodizime (HR 221) on immunological defects induced by surgical stress.

Cefodizime, a new aminothiazolylcephalosporin, has been shown to possess immunomodulating activity in many experimental models in vivo and in vitro. The in-vivo effect of the drug was evaluated in a model represented by the surgical patient, being surgical practices usually associated with an immunological impairment involving many aspects of the immune response. Two groups of ten subjects were treated respectively with cefodizime (2 g i.v. daily) and another cephalosporin (ceftriaxone) at the same dosage. Aspecific immunity (complement activity, neutrophil phagocytosis, chemiluminescence and superoxide anion production) and cell-mediated reactivity (lymphocyte subpopulations and E-rosette-forming cells) were evaluated before, and at predetermined intervals after, surgery and antibiotic treatment. In the control group an important immunological derangement is observed, involving both lymphocytes and neutrophil functions and complement system. The treatment with cefodizime displays a positive effect with a significant improvement of impaired functions. The effect of the drug particularly influences neutrophil phagocytosis, explored with both the NBT test and determinations of chemiluminescence, and the complement system, through both the classic and the alternative pathways. A slight effect is observed on lymphocyte functions.

Adolescent↗
PubMed1990

Proton tunneling in hydrated biological tissues near 200 K.

We measure the protonic conductivity in water clusters adsorbed on intact samples of viable biological samples (corn embryo and endosperm, Artemia cysts, and Typha pollen) below room temperature. In the low-temperature region, the conductivity increases with temperature as exp T6, in agreement with prediction by the theory of dissipative quantum tunneling. We detect the onset of this effect near 180 K, where a glass transition in the hydrated protein matrix is known to take place. Above 220 K other transitions are superimposed onto this simple behavior.

Animals↗
PubMed1990

Synthesis of 2-[1,2-dihydropyrazol-4-yl]-1,3,4-thiadiazole derivatives as potential antimicrobial agents.

The synthesis of some 2-[1,2-dihydropyrazol-4-yl]-1,3,4-thiadiazole derivatives is performed by reacting 4-dithiocarboxylic acid hydrazides of 3-amino-1,2-dihydro-5H-pyrazol-5-one and 3-amino-1,2-dihydro-1-methyl-5H-pyrazol-5-one with carboxylic acid derivatives. The unusual behaviour of 3-amino-1,2-dihydro-1-methyl-5H-pyrazol-5-one towards acetylating agents is described. The antimicrobial activity of some 2-[1,2-dihydropyrazol-4-yl]-1,3,4-thiadiazole derivatives is tested in a preliminary screening.

Anti-Bacterial Agents↗
PubMed1989

Dielectric properties of Artemia cysts at low water contents. Evidence for a percolative transition.

Cellular cysts of the crustacean Artemia provide a useful model for studies on water-dependent mechanisms in cellular function because they can undergo reversible cycles of dehydration-rehydration. We explored their dielectric behavior over the frequency range of 10 kHz to 1 MHz, at water contents between near zero and 0.5 g H2O/g dry weight (g/g). The dc conductivity and static dielectric permittivity were evaluated from electrostatic analysis of data obtained with a three-layered capacitor. Below cyst hydrations of 0.05 g/g, negligible dielectric response was observed at all frequencies. Between 0.05 and 0.25 g/g the permittivity increased sharply then reached a near plateau up to cyst hydrations close to 0.35 g/g, above which a second abrupt increase occurred. Values for the dielectric loss (tan delta) exhibited frequency-dependent peaks over the hydration range of 0.05-0.3 g/g, followed by an abrupt increase near 0.35 g/g, an hydration at which metabolism is first initiated in this system. These hydration-dependent dielectric changes are compared with previous studies on the biology and physics of this system, and evaluated by a model involving percolative ionic (likely protonic) conduction. Percolative behavior is characterized by a sharp increase in conductivity at a critical threshold of hydration (hc) according to a power law in which the exponent, t, equals 1.65 for a three-dimensional infinite lattice. For the Artemia cyst, t = 1.64 above hc = 0.35 g/g, which is in excellent agreement with theory. These results are compared to similar studies on lysozyme which also exhibits percolative behavior connected with the onset of biological function.

Animals↗
PubMed1987

Synthesis of some 7-phenylpyrrolo[1,2-a]pyrimidine derivatives. III.

2-Amino-4-phenylpyrrolyl-3-carbonitrile (I) was reacted with ethyl formylacetate sodium salt affording 1,4-dihydro-4-oxo-7-phenylpyrolo[1,2-a]pyrimidin-8-carbonitrile (II), which was alkylated with EtI to give (III), which in turn was hydrolyzed to (IV). Treatment of both (III) and (IV) with 99% H3PO4 at approximately 200 degrees gave 1,4-dihydro-1-ethyl-7-phenylpyrrolo-[1,2-a]pyrimidin-4-one (V) whose structure was ascertained by an unequivocal synthesis starting from (I) and diethyl ethoxymethylenmalonate. Compound (V) was prepared in order to test its pharmacological properties in comparison with 4,7-dihydro-4-ethyl-2-phenylpyrazolo[1,5-a]pyrimidin-7-one, which showed an antiinflammatory activity comparable to that of phenylbutazone and indomethacine, and which was found devoid of ulcerogenic properties.

Animals↗
PubMed1987

Pharmacological activity of some pyrrolo and pyrazolo pyrimidine derivatives.

4,7-Dihydro-4-ethyl-2-phenylpyrazolo-[1,5-a]pyrimidin-7-one (FPP028) is the prototype of a class of pyrazolo[1,5-a]pirimidine derivatives that has been shown to possess marked antiinflammatory and analgesic properties; 1,4-dihydro-1-ethyl-7-phenylpyrrolo[1,2-a]pyrimidin-4-one (FPP129) is a new compound belonging to a series of pyrrolo[1,2-a]pirimidine derivatives that has been synthetized in an attempt to reduce certain toxic effects observed with FPP028. To evaluate these two compounds more fully, in the present study we determined the LD50 of FPP129 in mice and assessed its activity in different experimental inflammation models. Ulcerogenic properties of FPP129 were evaluated by the test of stress-induced ulcer in rats. We also studied the in vitro and ex vivo effects of both FPP028 and FPP129 in a series of platelet-aggregation experiments using either arachidonate or collagen as aggregating agents. In the carraggeenan-induced paw edema, FPP129 exerted a marked anti-inflammatory activity with an ED50 of 22.2 mg/kg. FPP129 inhibited also the edema induced by concanavalin-A or Paf-acether. The in vitro anti-aggregatory activity of FPP028 was shown to be much less than that of indomethacin, thus confirming the hypothesis that the compound is a very weak inhibitor of cyclooxygenase. Ex vivo, both FPP028 and FPP129 were shown to exert no antiaggregatory effect in rabbits after administration of doses equal to the ED50. No ulcerogenic activity was found with FPP129, this result being consistent with previous observations on FPP028. Our data show tha FPP028 and FPP129 do not share a typical mechanism of action (cyclooxygenase inhibition) found with the majority of nonsteroidal antiinflammatory drugs. Nonetheless, the antiinflammatory properties of these compounds, together with their lack of ulcerogenic activity, indicate that both FPP028 and FPP129 are potentially interesting for future therapeutic use.

Animals↗
PubMed1986

Biofiltration with buffer-free dialysate.

The presence of acetate in the dialysate appears to be superfluous in the new depurative technique indicated as biofiltration, which consists in a standard hemodialysis with high ultrafiltration combined with the reinfusion of 3-4 1/2 liters of solution containing bicarbonate. The presence of acetate could in fact be contraindicated by a number of potential side effects, metabolic, cardiovascular and biological. Hence, starting from the consideration that in standard biofiltration a buffer is already infused directly as bicarbonate, we tried to overcome the potential hazards of the acetate-containing bath simply by using a dialysate without acetate and by increasing the concentration of bicarbonate in the reinfusate. A cumulative clinical experience of 20 months in 4 patients proved the feasibility and safety of the technique and suggests further advantages over standard biofiltration (better control of acid-base equilibrium, better cardiovascular stability.

Acetates↗
PubMed1986

[Some derivatives of the 2-[4-pyrazolinyl]-1,3,4-thiadiazole system].

The synthesis of some 2-[5-amino-1-methyl-3-oxo-4-pyrazolynyl]-1,3,4-thiadiazole derivatives is accomplished by reacting 5-amino-1-methyl-3-oxopryrazolynyl-4-dithiocarbohydrazide with carboxylic acid derivatives. The structure of the compounds obtained is verified by means of 1H and 13C-N.M.R. spectra. Antimicrobial and antifungal activity of some of the described compounds was tested in a preliminary screening.

Anti-Infective Agents↗
PubMed1983

2-Phenylpyrazolo[1,5-a]pyrimidin-7-ones. A new class of nonsteroidal antiinflammatory drugs devoid of ulcerogenic activity.

Syntheses of some pyrazolo[1,5-a]pyrimidines were performed in order to study the relationship between structural modifications on the parent 4,7-dihydro-2-phenylpyrazolo[1,5-a]pyrimidin-7-one (1) and their antiinflammatory properties. The modifications carried out were introduction and functionalization of a longer side chain at the 4-position, substitution of the hydrogen atom at the 3-position, and replacement of the phenyl group with a 4-methylphenyl, methyl, or hydrogen substituent. 4-Ethyl-4,7-dihydro-2-phenylpyrazolo [1,5-a]pyrimidin-7-one (3) showed the highest activity and a better therapeutic index than phenylbutazone and indomethacin, used as reference drugs. All other changes at the 3-, 5-, and 6-positions, as well as the replacement of the phenyl group at position 2, caused a marked decrease of activity. Compound 3 was found devoid of ulcerogenic activity and was probably endowed with antiulcerogenic properties.

Animals↗
PubMed1981

New pharmacologically active 2-phenylpyrazolo [1,5-a]pyrimidines.

2-Phenylpryrazolo [1,5-a]pyrimidine (I) 4,7-dihydro-2-phenylpyrazolo [1,5-a]pyrimidin-7-one (II) and 4,5-dihydro-2-phenylpyrazolo [1,5-a]pyrimidin-5-one (III) are prepared. Because of the interesting antipyretic, hypothermizing and anti-inflammatory properties of some of their derivatives, the above mentioned compounds are used as reference compounds in a Q.S.A.R. study still in progress. Methylation of (II) and (III) with (CH3)2SO4 and CH2N2 gives methylderivatives whose structure is determined by spectroscopic means.

Animals↗