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Biomedical subjects

L Bastianini

Publications and source records attributed to L Bastianini.

At least 19 recordsLinked to original sources

New heterocyclic derivatives of benzimidazole with germicidal activity--IX--HPLC detection of 5-fluoro-2-(5'-nitro-2'-furyl)benzimidazole (F-O-NO2) in biological samples.

The HPLC technique for the isolation and quantitation of 5-fluoro-2-(5'-nitro-2'-furyl)benzimidazole (F-O-NO2), previously described by the same Authors, in biological samples from mice is reported. Evidence is given that the highest biological concentration and the time needed for reaching it depend both on the dose and on the administration route. In fact, almost the same maximal biological concentration of F-O-NO2 (about 0.18 micrograms/mouse) is reached after 60 min from either 40 mg/Kg IP or 200 mg/Kg os drug administration, whereas the maximal biological concentration of F-O-NO2 (5.75 micrograms/mouse) is reached after 30 min from 120 mg/Kg IP drug administration.

Animals

New heterocyclic derivatives of benzimidazole with germicidal activity--VII--2-(5'-nitro-2'-furyl or 2'-thienyl) benzimidazoles with different substituents in the 5-position.

In continuation of our previous research, the synthesis of 13 2-(5'-nitro-2'-furyl or 2'-thienyl) benzimidazoles with different substituents in 5 position is described. The new compounds were tested in vitro against 5 (Gram+) and 4 (Gram-) strains and a mycete Candida Albicans. All the derivatives showed a certain degree of antibacterial and antimycotic activity, which in some cases was fairly good.

Anti-Bacterial Agents

Chemometric approach in a QSAR study: the antibacterial and antimicotic activities of benzofused heteroaromatic derivatives.

In order to establish quantitative relationships between the antibacterial activities of a number of thienyl- and furyl-benzimidazoles and benzoxazoles, the biological data were measured homogeneously for a selected set of 16 representative compounds of the available set of 103. The data were analyzed by the PLS method. The results of linear PLS modelling and PLS response surface modelling permitted a straightforward interpretation of the structural features relevant to the activities and the prediction of a possible optimal structure.

Anti-Bacterial Agents

[New heterocyclic derivatives with germicidal activity. VI. Synthesis and activity of new 2-benzoxazoyl-2'-furanes and -thiophenes variously substituted in 5 and 5' positions].

Seventeen derivatives of 2'-furyl-2-benzoxazole and three derivatives of 2'-thienyl-2-benzoxazole, having different substituents in the benzene moiety (position 5) and in the furanic or thiophenic ring (position 5'), are described, with the aim of studying antibacterial and antimycotic structure-activity relationships. None of the compounds show an important antibacterial and/or antimycotic activity, when tested against nine bacteria and Candida albicans cultures; in any case it was much lower than that previously reported for the corresponding benzimidazoles. It seems that the = NH group of the imidazole ring, which is absent in the benzoxazole derivatives, might be important for the biological activity of this class of compounds.

Anti-Bacterial Agents

Microbial flora of surface versus core tonsillar cultures in recurrent tonsillitis in children.

Surface and 'core' tonsillar specimens were collected from 60 children, between 2 and 14 years of age, suffering from recurrent tonsillitis, in order to establish the reliability of surface tonsillar swabbing technique and to define the most frequently involved aerobic and anaerobic microorganisms. From the qualitative point of view, the same mixed aerobic and anaerobic flora were obtained in both samples thus demonstrating the reliability of the surface swabbing technique. From the quantitative point of view, 187 microorganisms, 129 (69.2%) aerobes and 58 (30.8%) anaerobes were isolated from surface cultures while 184, 109 (59.2%) aerobes and 75 (40.8%) anaerobes from the core cultures, thus demonstrating a greater number of anaerobes in the core of the tonsil. The most common isolated aerobic microorganisms were the alpha- and beta-hemolytic Streptococci, the Neisseriae and the Staphylococcus aureus; the predominant anaerobic ones were the Fusobacterium nucleatum, the Bacteroides sp. and the Veillonella parvula. The isolated staphylococcus aureus and the bacteroides sp. were all beta-lactamase producers.

Adolescent

Comparative in vitro activity of imipenem against gram-positive and gram-negative aerobic bacteria from clinical isolates.

Imipenem is a member of a new class of beta-lactam antibiotics, carbapenems, with a very broad antibacterial spectrum. In this work we evaluated the in vitro activity of imipenem against a variety of bacterial strains isolated from clinical specimens as well as the activity of other beta-lactam antibiotics. The results obtained with 501 bacterial strains show that imipenem is active on both gram-negative and gram-positive microorganisms isolated from different infections. The in vitro inhibitory activity is greater than that of aztreonam, cefotaxime, ceftriaxone, piperacillin, amikacin, and netilmicin, against the majority of strains tested.

Anti-Bacterial Agents

[New heterocyclic derivatives of benzimidazole with germicidal activity. V. Synthesis and activity of new derivatives of di-2-benzimidazolyl-2,5-furan].

In continuation of the research in the field of germicidal and antimycotic agents, the synthesis of 14 new derivatives of di-2-benzimidazolyl-2,5-furan is described. These derivatives are differently substituted (R not equal to R') in the position 5 of the two benzene rings. These new compounds showed no germicidal or fungicidal activity, when tested on different cultures. New compounds are under investigation.

Anti-Infective Agents

New heterocyclic derivatives of benzimidazole with germicidal activity. IV--In vivo anticandida activity of 5-fluoro-2-(5'-nitro-2'-furyl) benzimidazole (F-O-NO2).

We have studied the possible in vitro and in vivo antibacterial activity of 5-fluoro-2-(5'-nitro-2'-furyl)benzimidazole (F-O-NO2). Our data demonstrate that F-O-NO2 is able to inhibit the in vitro growth of different mycetes and bacteria, including Candida albicans and Cryptococcus neoformans. We also tested the possible in vivo activity against Candida albicans. The results clearly show that treatment with F-O-NO2 is able to significantly augment the survival of all treated animals; in particular, when injected i.p. at the dose of 120 mg/kg, 30' or 1 hr after Candida albicans challenge, it givens a MST (Medium Survival Time) longer than 60 days. These data demonstrate that F-O-NO2 has antibacterial and antimycotic activity.

Animals

Microbial flora of nose and paranasal sinuses in chronic maxillary sinusitis.

Nasal secretions, maxillary sinus aspirates and specimens of the maxillary sinus mucosa were collected in 44 patients aged between 25 and 60 affected by mono- or bilateral chronic maxillary sinusitis, in order to establish the best sampling technique for microbiological purposes, the most frequently involved bacteria and the physiopathological mechanism underlying chronic maxillary disease. The sinusal mucosa resulted to be the most reliable sample as it reduces contamination and microbial variability. Anaerobic bacteria were isolated in nasal swab (15.6%), in maxillary sinus aspirates (30.4%) and in maxillary sinus mucosa (36.4%) of maxillary sinusitis patients. In controls anaerobic bacteria were isolated only in one nasal swab (2.3%), while they could not be isolated in maxillary sinus aspirates and in maxillary sinus mucosa. The presence of anaerobic bacteria in chronic maxillary sinusitis patients and their absence in controls seem to confirm that anaerobic microorganisms represent the main pathogenetic agents of chronic maxillary sinusitis. The possible physiopathological mechanisms underlying chronic maxillary sinus disease are finally discussed.

Adolescent

[New heterocyclic derivatives of benzimidazole with germicidal activity. III. Synthesis and activity of derivatives of (formyl-5'-furyl-2')-2-benzimidazole with different substitutions at position 5].

The synthesis and germicidal properties of 28 new derivatives of furyl-2-benzimidazole are described. The compounds are substituted both in position 5 of the benzene moiety and in position 5' of the heterocycle moiety. The germicidal properties of the new molecules were tested using 9 strains of bacteria and Candida albicans. Some of them exhibited germicidal properties versus Gram + bacteria and versus Candida. Some derivatives were also tested using Mycobacterium aurum: two isonicotinoylhydrazones derivatives exhibited tubercolostatic activity comparable to that of streptomycin and not much lower than that of isoniazide.

Anti-Bacterial Agents

Turkey red blood cell passive haemagglutination assay as guideline for specific prevention of tetanus in injured persons.

Turkey red blood cell passive haemagglutination assays (TRBC-HA) were carried out on serum samples from 873 injured patients in order to compare individual prophylactic treatment against tetanus based on the anti-tetanus antibody levels with interventions based on anamnestic criteria. The results showed a great difference: according to the anamnesis 124 persons (14.2%) were protected, 253 (29%) were partially protected, and 496 (56.8%) were unprotected; according to the TRBC-HA assay, 479 (54.9%) were protected, 279 (32%) partially protected, and 115 (13.2%) unprotected.The efficiency of the prophylactic treatments given on the basis of the two criteria was also compared in a study of 129 injured patients who were divided in two groups: group 1 (50 patients) received 250 IU of human tetanus immunoglobulin (HTI) regardless of their tetanus immunity, and group II (79 patients) received appropriate or no treatment depending on the level of anti-tetanus antibodies determined by TRBC-HA assay. The results showed that prophylactic interventions based on the anti-tetanus antibody levels can give protection in 100% of injured patients at minimum cost and risk.

Animals

The state of antitetanus protection in the commune of Perugia.

A serological survey was carried out on the population in the Perugia district to assess the protection level against tetanus. The antitoxin titre was evaluated by indirect haemagglutination test in 983 sera from healthy subjects of both sexes and all age-groups. Only 285 males and 144 females, 33.47% of the subjects, had been immunized prior to the investigation. The research made it clear that the serological antibody level does not always correspond to the anamnestic data on previous immunization. Therefore, it appears that prophylactic treatment against tetanus should be based on objective data, that is, serum antibody titre, in all subjects at risk. This information, thanks to the indirect haemagglutination test, is not difficult to obtain.

Adult

Haemagglutination antibody titre levels which give certain protection against tetanus toxin.

The lowest haemagglutination titre which gives safe protection against tetanus toxin, in sera of vaccinated subjects of both sexes and of all age groups has been assessed, by comparative haemagglutination and neutralization tests. It was established that sera with 1/32 haemagglutination antibody titre have a toxin neutralizing capability of greater than or equal to 0.1 I.U./ml. Lower haemagglutination titers do not assure protective capacity against tetanus toxin.

Animals

Serum antibody level in rabbits submitted to antitetanus active-passive immunization with heterologous horse serum.

Serum antibody titres have been assessed in rabbits submitted to active and active-passive immunization against tetanus with AlPO4 adsorbed vaccine and horse heterologous immune serum. Heterologous antibodies survive in the blood stream no more than six days. Endogenous antibodies, with the adopted vaccination schedule, emerge fifteen days after the first vaccine inoculation. In rabbits undergoing active-passive immunization, the appearance time of endogenous antibodies is delayed, all the more so as the antiserum injected dose increases. Such data stress the opportunity to give up with the use of heterologous immune sera in tetanus prophylaxis, in association with vaccine as well.

Animals