Biomedical subjects

S Massa

Publications and source records attributed to S Massa.

At least 91 records · Page 5Linked to original sources

PubMed1990

Synthesis and antimicrobial and cytotoxic activities of pyrrole-containing analogues of trichostatin A.

A number of aroylpyrroleacrylic acid derivatives were synthesized by standard procedures and evaluated for cytotoxicity in Vero cells and for capacity to inhibit the multiplication of viruses, bacteria, and fungi. While none of the test compounds showed any activity against bacteria and fungi, most of them inhibited the replication of some DNA viruses at concentrations allowing the exponential growth of uninfected cells. In particular three compounds (8, 9c, and 10h) showed an antiviral activity at doses that were from 4- to greater than 8-fold lower than the maximum nontoxic doses.

Animals↗

PubMed1990

The incidence of Listeria spp. in soft cheeses, butter and raw milk in the province of Bologna.

Samples of soft cheese, butter and raw milk were examined for Listeria species. Listeria monocytogenes (serotype 1, haemolytic and virulent for mice) and L. innocua (the only other Listeria sp. isolated) were each found in 2/21 (1.6%) of soft cheese samples. Five per cent of butter samples were contaminated with L. innocua. No Listeria spp. were detected in 40 raw milk samples. The results were compared with similar studies in Italy and abroad.

Animals↗

PubMed1990

Pyrrolobenzodiazepine and related systems. I. Synthesis and pharmacological evaluation of new 5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepine derivatives.

Some new 5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepine derivatives substituted at the 5 position have been synthesized and tested to evaluate their antidepressant and neuropsychopharmacological activities. The antinociceptic action of these compounds has been also assayed. The introduction of an ethoxycarbonyl group at the 4 position generally decreased the antidepressant effect.

Analgesics↗

PubMed1990

Preliminary results corroborating the polygenic control of immunological tolerance.

Tolerance-susceptible (TS) and -resistant (TR) lines of mice are in the process of bidirectional genetic selection starting from a genetically heterogeneous population achieved by the equilibrated intercrossing of eight inbred lines. Mice are intragastrically pretreated and then immunized with hen ovalbumin or bovine serum albumin and the extreme phenotypes are selected for assortative mating. The normal distribution of agglutinin titers in the F0 population and the significant interline difference already observed in the F2 and F3 generations indicate that oral tolerance is a character controlled by the additive effect of several independent loci. The mean heritability (h2) obtained thus far is 11% for the TS line and 19% for the TR line.

Animals↗

PubMed1990

Research on antibacterial and antifungal agents. XIII. Synthesis and antimicrobial activity of 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylic acids.

Several 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylic acid derivatives have been synthetized and tested as antifungal and antibacterial agents. Reaction between tosylmethylisocyanide (TosMIC) and beta-arylacrylic esters under basic conditions furnished 4-aryl-1H-pyrrole-3-carboxylic esters, which were then benzylated at 1 position. Alkaline hydrolysis of ethyl 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylates afforded the title compounds. All tested derivatives were found to be inactive as antifungal agents. Some of them showed appreciable antibacterial activities against Staphylococcus spp.

Anti-Bacterial Agents↗

PubMed1989

Researches on antibacterial and antifungal agents, X. Synthesis and antifungal activities of 1-(p-methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)azoles and some related products.

The synthesis and antifungal activities against Candida albicans and Candida spp. of some pyrrole analogues of bifonazole are reported. 1-(p-Methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)imidazole was found to be equipotent or sometimes superior to bifonazole and ketoconazole, and lightly inferior to miconazole. Substitution of the imidazole moiety with other azoles retained some activities. No activity was shown when the azole aromatic rings were replaced by the heteroalicyclic ones.

Antifungal Agents↗

PubMed1989

Salmonella typhimurium infection in high and low antibody responder mice: inverse correlation between antibody responsiveness and resistance to infection.

Susceptibility to Salmonella typhimurium infection was compared in H (high Ab responder) and L (low Ab responder) mice obtained by several selective breeding experiments (Selections I, II, III, IV and IV A). H mice were always much more susceptible to infection than their L mice counterparts within a continuous LD 50 variation range. In three of the selections (I, II and IV A) the low responsiveness character is known to result mainly from rapid Ag degradation in L mice macrophages. It was hypothesized that resistance to multiplication of intracellular pathogens could be related to an increased catabolic activity towards Ag. This was actually demonstrated, in F2 segregant hybrids of selection IV A, by the significant inverse correlation between capacity for Ab production and resistance to infection.

Animals↗

PubMed1989

Synthesis, neuropsychopharmacological effects and analgesic-antiinflammatory activities of pyrrole analogues of lefetamine.

The synthesis of pyrrole analogues of the analgesic drug lefetamine is reported. These derivatives bear the 1-phenyl-2-(1H-pyrrol-1-yl)ethylamino moiety. Compounds were evaluated for analgesic activities in mice by the hot plate and Randall-Selitto tests. Antiinflammatory activity was tested by the carrageenan-induced rat paw edema method. General neuropsychopharmacological effects were also screened. The most interesting compound, N,N-dimethyl-1-phenyl-2-(1H-pyrrol-1-yl)ethylamine, showed an analgesic effect comparable to that of lefetamine, but devoid of the neurotoxicity of this drug.

Animals↗

PubMed1989

Research on antibacterial and antifungal agents. XI. New antibacterial quinolones related to pirfloxacin.

The synthesis and antimicrobial activities against Gram-positive and Gram-negative bacteria of some 1-substituted quinolones related to pirfloxacin are reported. Compounds with a benzyl moiety at 1-position were generally found to be less active than the analogues bearing an unsaturated alkyl chain at the same position. Introduction of fluorine or chlorine in the benzyl moiety did not increase the antibacterial activity. All derivatives here reported were inferior to pirfloxacin as regards antibacterial power, but always superior in comparison with nalidixic acid and pipemidic acid against Gram-positive microorganisms.

Anti-Infective Agents↗

PubMed1989

[5-Aroyl-5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepin-4-carboxylic acids: synthesis and analgesic and neurobehavioral activity].

Reaction between 1-(2-aminomethylphenyl)-1H-pyrrole hydrochloride and methyl 2-methoxyglicolate in methanol afforded methyl 5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepin-4-carboxylate. Aroylation at the 5-position and subsequent hydrolysis of the ester function led to 5-aroyl-5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepin-4-ca rboxylic acids. The pharmacological profile of these acids has been studied with regard to analgesic, antiinflammatory and neuropsychobehavioural effects.

Analgesics↗

PubMed1988

Spectroscopic studies of the reaction between bovine serum amine oxidase (copper-containing) and some hydrazides and hydrazines.

The carbonyl cofactor of bovine serum amine oxidase, recently identified as pyrroloquinoline quinone [Ameyama, Hayashi, Matsushita, Shinagawa & Adachi (1984) Agric. Biol. Chem. 48, 561-565; Lobenstein-Verbeek, Jongejan, Frank & Duine (1984) FEBS Lett. 170, 305-309], reacts stoichiometrically and irreversibly with hydrazides of phenylacetic acid and of benzoic acid. With the phenylacetic hydrazides a reversible intermediate step was detected by competition with substrate, carbonylic reagents or phenylhydrazine, a typical inhibitor of the enzyme. All hydrazides form an intense broad band with maximum absorbance in a narrow wavelength range (350-360 nm), irrespective of the acyl group, suggesting that the transition is located on the organic cofactor. A different situation is found with some phenylhydrazines, where extended conjugation can occur between the cofactor and the phenyl pi-electron system via the azo group, as shown by the lower energy and higher intensity of the transition. In this case the transition is sensitive to substituents in the phenyl ring. The c.d. spectrum of the adducts is influenced by the type of hydrazide (derived from phenylacetic acid or benzoic acid), by pH and by NN-diethyldithiocarbamate binding to copper, probably as a result of shifts of equilibria between hydrazone-azo tautomers.

Amine Oxidase (Copper-Containing)↗

PubMed1988

Polygenic control of quantitative antibody responsiveness: restrictions of the multispecific effect related to the selection antigen.

Among the differences observed between the various high (H) and low (L) antibody responder lines of mice resulting from distinct bidirectional selective breedings, one of the most puzzling is the variation in the "multispecific effect," i.e., in the modification of antibody responses to antigens unrelated to those used during the selection. The best examples are the H and L lines of selection IV, selected on the basis of responses to somatic antigen of Salmonella which do not differ in their antibody responses to sheep erythrocytes (SE). However, a wide range of variability is observed in the responses of (HIV X LIV)F2 hybrids to this antigen, and it was therefore hypothesized that distinct groups of genes might regulate antibody responses to SE and the somatic antigen. Indeed, a new selection (IV-A) for anti-SE responsiveness started from these (HIV X LIV)F2 successfully produced a high and a low anti-SE responder line. The results of selection IV-A and the variance analysis of (HIV-A X LIV-A)F2 hybrids are reported. They are roughly similar to those in selection I, also carried out for anti-SE responsiveness. In vivo attempts to identify the major regulatory mechanism which contributes to the interline difference indicate that the efficiency of macrophage accessory function has been modified in selection IV-A, as was observed in selection I, whereas this function did not differ in HIV and LIV lines. Probably in relation to the involvement of macrophage function there is a notable increase of the multispecific effect in selection IV-A when compared with selection IV. The results of selection IV-A demonstrate that responsiveness to heterologous erythrocytes and to somatic antigen of Salmonella are under separate polygenic control operating through distinct regulatory mechanisms. The choice of the selection antigen and immunization procedure is of major importance for defining the gene interaction operating in each selective breeding experiment and the extent of its multispecific effect.

Animals↗

PubMed1988

Microbiological quality of fresh pasta dumplings sold in Bologna and the surrounding district.

The microbiological quality of fresh pasta dumplings sold in Bologna and the surrounding district was evaluated. A total of 60 lots (300 subsamples) of fresh pasta dumplings, both 'home-made' and manufactured, were analysed for aerobic plate count (APC), coliforms (total and fecal), Staphylococcus aureus, Clostridium perfringens and Salmonella spp. Thirty one of the 39 lots of 'home-made' pasta were found to exceed APC standards and six lots exceeded S. aureus standards. Five (24%) and six (29%) lots of the manufactured pasta were found to be unsatisfactory as regards APC standards and S. aureus standards respectively. The results obtained indicated that a high percentage of samples had a contamination of fecal origin. No Cl. perfringens or Salmonella spp. were found.

Bacteria↗

PubMed1988

Inhibition of copper-dependent amine oxidases by some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids.

Some hydrazides of pyrrol-1-ylbenzoic and pyrrol-1-ylphenylacetic acids were prepared, and their effect on copper-dependent amine oxidases (Cu-AOs) and FAD monoamine oxidases (MAOs) activities was tested. The compounds were not substrates for Cu-AO enzymes but acted as noncompetitive inhibitors. Hydrazides of pyrrol-1-ylphenylacetic acids were highly specific for plasma amine oxidase (Ki = 0.5-1 microM). In contrast, all the hydrazides were weak inhibitors of MAO activity. Incubation with the hydrazide derivatives led to irreversible inactivation of Cu-AOs. Therefore, the inhibition implied two distinct steps. The first one consisted of the rapid formation of the enzyme-inhibitor complex and was reversed by dialysis. In the second step, the complex was irreversibly transformed, probably by the formation of a Schiff base between the hydrazide and the prosthetic carbonyl group of the enzyme.

Amine Oxidase (Copper-Containing)↗

PubMed1988

Researches on antibacterial and antifungal agents. IX--Pyrrole analogues of bifonazole with potent antifungal activities.

The synthesis and antifungal activities of pyrrole analogues of bifonazole are reported. Reduction of 4-nitrobenzophenone to the corresponding alcohol, reaction with phosphorus tribromide of the latter compound and condensation of the bromonitroderivative with imidazole led to 1-[alpha-(4-nitrophenyl)-4'-benzyl]-1H-imidazole. Hydrogenation of the nitro group to amino and reaction with 2,5-dimethoxytetrahydrofuran according to the Clauson-Kaas procedure afforded the pyrrole analogue of bifonazole. This compound and the related chloroderivative were also prepared by a similar pathway starting from 4-(1H-pyrrol-1-yl)benzophenone and its 4'-chloroderivative. Microbiological screening against Candida albicans and Candida spp showed 1-(alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)-1H-imidazole to be the most active compound among the tested derivatives.

Antifungal Agents↗

PubMed1988

Isolation of Yersinia enterocolitica and related species from river water.

One hundred and twenty samples of river water collected from sampling sites in the period between December 1986 and December 1987 were examined for the presence of Yersinia enterocolitica and related species. Among a total of 26 Yersinia strains isolated the following species were recognized: Y. enterocolitica, 12 strains, Y. intermedia, 5 strains, Y. frederiksenii, 2 strains, Y. kristensenii and Y. aldovae, 1 strain each; 5 were atypical Yersinia strains (rhamnose+, citrate+, alpha-methyl-D-glucoside+). Although the Yersinia isolates belong to the so-called "environmental" serotypes, which are usually considered as non-pathogenic for humans, Y. enterocolitica biotype 1, serotype 0:7.8, lysotype X0, which has previously been associated with gastro-intestinal infection in Italy, was found to be present. Statistical evaluation of our data showed that the presence of Yersinia spp. and the presence of total or fecal coliforms are unrelated.

Colony Count, Microbial↗

PubMed1988

[Nonsteroidal anti-inflammatory agents. V. Synthesis of 1-aryl-5-(1-pyrryl)-pyrazolyl-4-acetic acids with potential anti-inflammatory action].

The synthesis of 1-aryl-5-(1-pyrryl)pyrazoles bearing at position 4 an acetic or alpha-propionic chain is described. The new compounds can be structurally related to lonazolac and its analogues with analgesic-antiinflammatory activities. When tested pharmacologically in comparison with tolmetin and indomethacin none of the above derivatives showed any appreciable activity.

Acetates↗

PubMed1987

[Research on antibacterial and antifungal agents. VII. Synthesis of (1-pyrryl)methylquinolines acids].

Some (1-pyrryl)methyl derivatives of 1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid were synthetized by the standard procedure involving Gould-Jacobs and Lappin reactions. The above derivatives were tested microbiologically as nalidixic acid analogs and compared with some clinically useful 4-oxopyridine-3-carboxylic acids (nalidixic acid, pipemidic acid, norfloxacin, enoxacin and ciprofloxacin). Their antibacterial activities were very weak.

Anti-Bacterial Agents↗