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Biomedical subjects

A Costanzo

Publications and source records attributed to A Costanzo.

At least 73 records · Page 4Linked to original sources
PubMed1993

Synthesis and study of the anti-inflammatory properties of some pyrazolo[1,5-a]pyrimidine derivatives.

A series of pyrazolo[1,5-a]pyrimidin-7-ones (1c-17c) were synthesized to evaluate in vivo and in vitro effects induced by structural modifications at the 2 position of 4,7-dihydro-4-ethyl-2-phenylpyrazolo[1,5-a]pyrimidin-7-one (FPP028). This substance, which has been previously studied, is a weak inhibitor of prostaglandin biosynthesis and a nonacid analgesic and anti-inflammatory agent devoid of ulcerogenic properties. To gain more insight into the mechanism of action of this class of compounds, several in vivo tests were carried out, such as carrageenan-induced rat paw edema and pleurisy. In vitro tests include some studies of leukocyte functions, such as superoxide production and myeloperoxidase release. In vitro effects on arachidonic acid-, adenosine 5'-diphosphate-, and platelet-activating factor-induced platelet aggregation were also studied. Different anti-inflammatory activities were observed, depending on the nature of substituents at the 2 position; these differences are probably linked to the capacity of these compounds to inhibit leukotrienes and/or prostaglandin biosynthesis with different selectivity. 4,7-Dihydro-4-ethyl-2(2-thienyl)pyrazolo[1,5-a]pyrimidin-7-one (7c) proved to be the most interesting compound of the novel synthesized series, showing powerful pharmacological activity in vivo as well as in vitro, together with very weak acute toxicity.

Animals↗
PubMed1993

Detection of replicative intermediates of viral RNA in peripheral blood mononuclear cells from chronic hepatitis C virus carriers.

Clinical and experimental evidence suggests the possible existence of one or more extrahepatic sites of HCV infection. In order to demonstrate the "in vivo" infection of lymphoid cells by HCV, we applied a nested PCR to total cytoplasmic RNA extracted from fresh or cultured peripheral blood mononuclear cells (PBMCs) of HCV chronically infected patients, using primers derived from the highly conserved 5' untranslated region of the HCV genome. The presence of virions in PBMCs occurs frequently, if not always, and is often accompanied by active viral replication. Moreover, the appearance of replicative intermediates after stimulation of cellular growth with mitogens suggests that latent genomes could undergo replication upon cellular activation and/or proliferation.

Adult↗
PubMed1993

Synthesis of 7-(2-dimethylaminovinyl) derivatives of pyrazolo[1,5-a] pyrimidines, as precursors of new tricyclic series. Binding studies of BDZ receptor.

A series of 7-dimethylaminovinylpyrazolo[1,5-a]pyrimidines bearing an acetyl or an ethoxycarbonyl group at the 6-position turned out to be useful intermediates for the synthesis of pyrazolo[1,5-a]pyrido[3,4-e]pyrimidines and 8H-pyrazolo[5',1':2,3]pyrimido[5,4-d][1,2]diazepines. These tricyclic derivatives were studied for their affinity for the central benzodiazepine receptor, and meaningful suggestions about the structure-affinity relationship were obtained. Some of the above intermediates were also reacted with S-methylthiourea, to give a mixture of pyrazolo[5',1':1,2]pyrimido[5,6-e][1,3]diazocines and pyrazolo[1,5-a]quinazolines.

Binding, Competitive↗
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↗
PubMed1987

Impeded eruption rate of the rat maxillary incisor during exposure to different simulated altitudes.

Female rats weighing about 200 g each were separated into normoxic and hypoxic groups. The former were maintained at sea-level conditions. The hypoxic groups were placed in an altitude chamber and maintained at the equivalent of 1850 m, 4100 m, or 7100 m over a period of two weeks. Hematocrit, body weight, body length, and impeded eruption rate were recorded once a week. Food intake was recorded every day. Exposure to 1850 m did not significantly alter hematocrit, body weight and body length gains, food intake, and impeded eruption rate. Nevertheless, exposure to 4100 m and 7100 m decreased body weight and body length gains, food intake, and impeded eruption rate, and increased hematocrit value. These parameters varied as a function of altitude. In spite of the lack of conclusive evidence, this work affords further insight into the particular significance of polycythemia on the eruption rate.

Altitude↗
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

[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↗
PubMed1985

[Potential ratios among blood levels of various blood proteins in the cord blood of healthy newborn infants].

The authors have studied the correlations between IgA, IgG, IgM, C3c, C4, alpha 1-AGP and the total proteins, total globulins, alpha 1, alpha 2-globulins in normal newborn cord blood. The results indicate some significant correlations between C3c and C4, C3c, C4 and alpha 1-AGP, C3c, C4, alpha 1 1/2AGP and alpha 2-globulins, C4 and beta-globulins, C3c and alpha 1-AGP. The most significant finding has been inverse correlation between IgA and alpha 1, alpha 2-globulins, total globulins and total proteins.

Alpha-Globulins↗
PubMed1984

[Effects of the use of FRIGEN (AG-Ffm-HOECST) on the determination of blood levels of some proteins (IgA, IgM, IgG, C3c, C4) in cord blood of healthy newborn infants at term by laser nephelometry].

The purpose of this paper is to establishes the FRIGEN effects on the determination of IgA, IgM, IgG, C3c, C4 cord-blood levels, by means of laser-nephelometry. The results show substantial interferences only in the IgA levels, whereas the other on almost all proteins are not affected, the found interference can be due to the amount of IgA bound to B-lipoprotein, that are precipitated by FRIGEN.

Chlorofluorocarbons, Methane↗