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Biomedical subjects

N Simonetti

Publications and source records attributed to N Simonetti.

At least 73 records · Page 4Linked to original sources

[Antibacterial and antifungal compounds. V. Synthesis and antimicrobial activity of N-(2-arylethylaminophenyl)-1H-pyrryl-1-amine and 1-(1H-pyrrol-1-yl)-2-arylmethylbenzimidazole)].

The synthesis and antimicrobial activities of derivatives of 1-anilinopyrrole and 1-pyrrylbenzimidazole are described. The compounds here reported can be related to chlormidazole and other antifungal imidazole agents. The antifungal activity of the new derivatives tested proved lower than that of ketoconazole; some compounds were practically inactive.

Aniline Compounds↗

Pyrrolnitrin analogues. XI--Synthesis and microbiological activity of new 1,4- and 1,5-diarylpyrroles.

The synthesis and microbiological activities of new 1,4- and 1,5-diarylpyrroles is reported. Antimicrobial data in comparison with fungal antibiotic pyrrolnitrin confirm an interesting antimicotic activity of 1,4-diarylpyrroles. On the contrary 1,5-diarylpyrroles show antibacterial activity and an unexpected antimicotic activity. The position of the 4-nitrophenyl group at C4 or C5 of the pyrrole ring influences antibacterial activity.

Anti-Bacterial Agents↗

Serum lysozyme increased by fructose-1, 6-diphosphate in men, rabbits, and mice.

Fructose-1, 6-diphosphate hydrated sodium salt (FDP), intravenously injected, remarkably stimulates the production of serum lysozyme in man, rabbit, and mouse with a different kinetics in each of them: Man and rabbit show, in the first hour, a concentration peak followed by a slow decrease, whereas in mouse the concentration is less variable with time.

Animals↗

In vitro and in vivo antifungal activity of the combination methylpartricin-5-fluorocytosine.

In vitro studies on the antifungal activity exerted by the combinations SPA-S-222 (a hydrosoluble derivative of the polyene antibiotic methylpartricin) and 5-fluorocytosine evidence a favourable interaction against the formation of germ-tube in Candida albicans; against Cryptococcus neoformans and 5FC induced-resistant strains of Candida albicans. In the experimental infections with Candida albicans and Cryptococcus neoformans a significantly favourable interaction was exerted by polyene-5FC combinations.

Animals↗

Researches on antibacterial and antifungal agents. II - Synthesis of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid, a novel highly active, broad-spectrum antibacterial agent related to piromidic acid.

The synthesis and antibacterial activities of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrrolidinyl)quinoline-3-carboxylic acid are reported. The new analog of nalidixic acid has been prepared by standard procedure starting from 1-(3-aminophenyl)pyrrole; it showed a broad spectrum of antibacterial activity and exhibited much higher activity than nalidixic, pipemidic and piromidic acids. The synthesis of 1-ethyl-1,4-dihydro-4-oxo-8-(1-pyrrolyl)quinoline-3-carboxylic acid is also described; this acid was inactive when tested as antibacterial agent.

Anti-Bacterial Agents↗

Research on antibacterial and antifungal agents. III. Synthesis of 1-ethyl-1,4-dihydro-4-oxo-7-(1-pyrryl)quinoline-3-carboxylic acid and of some 6-derivatives.

A new analog of nalidixic acid, 1-ethyl-1,4-dihydro-4-oxo--7-(1-pyrryl)quinoline-3-carboxylic acid, is described. When tested against gram-positive and gram-negative bacteria this compound showed many significant activities and was more active than nalidixic, piromidic and pipemidic acids. On the contrary its 6-chloro- and 6-methylderivatives lack antimicrobial activities. All new compounds here described were synthesized by standard procedures via Gould-Jacobs reaction.

Anti-Bacterial Agents↗

Researches on antibacterial and antifungal agents. I. Analogs of nalidixic acid with a pyrrole moiety.

The synthesis and antibacterial activities of 4-hydroxyquinoline-3-carboxylic acid and 1,4-dihydro-1-ethyl-4-oxoquinoline-3-carboxylic acid containing a pyrrole or 2,5-dimethylpyrrole group at 6 position are reported. Reaction of 1-(4-aminophenyl)pyrrole or 2,5-dimethyl-1-(4-aminophenyl)-pyrrole with ethoxymethylenemalonate diethyl ester (EMME) afforded the related pyrroleanilinomethylenemalonates, which were subjected to thermal cyclization to give the required quinoline derivatives. These compounds on ethylation furnished at last the quinolonecarboxylic analogs of nalidixic acid.

Anti-Bacterial Agents↗

[Effect of propyl gallate on the antibacterial activity of meclocycline sulfosalicylate].

Propyl gallate shows little antibacterial activity however it markedly potentiates the activity of meclocycline against Pseudomonas, Proteus, Serratia, Escherichia coli and Klebsiella strains. The potentiating effect of propyl gallate is seen especially with resistant strains whereas sensitive strains of Salmonella do not manifest a potentiating effect on meclocycline by propyl gallate. The mechanism of action of propyl gallate is discussed.

Bacteria↗

Effect of a tetracycline antibiotic on the experimental pathogenicity of Cryptococcus neoformans.

The pathogenicity of three stains of Cryptococcus neoformans was experimentally tested by intradermal inoculations into albino rabbits and intraperitoneally into mice. A relationship was found between the number of inoculated cells and the diameter of dermal lesion; moreover, a typical kinetics of lesion evolution and healing has been shown. Treatment of rabbits with deoxytetracycline did not dramatically influence the behavior of dermal lesions. However, in experiments dealing with strain Vi selected for its enhanced dermotropism, the antibiotic did significantly provoke a diminition of the inflammatory area. In mice, the antibiotic caused a marked increase in mortality (as evaluated by both LD50 values and rate of mortality). Neither in rabbits nor in mice, however, were we able to detect a significant effect of the drug on the dissemination of C. neoformans cells in internal organs. There is no simple explanation for the reported observations but it is possible that local factors in the derma or an aspecific antiinflammatory action of deoxytetracycline are responsible for the unusual response of dermal experimental infection to antibiotic treatment.

Animals↗

Antimycotic activity in vitro and in vivo of a new hydrosoluble polyene antibiotic.

The in vitro and in vivo activity of a new water soluble polyene antibiotic, anmed SPA-S-222, has been studied on numerous Candida and Cryptococcus species. The in vitro tests were carried out in comparison with nystatin and amphotericin B whose antimycotic properties are already well known. The inhibition of "germination" of various strains of Candida albicans was also investigated. The results show that SPA-S-222 has greater antimycotic activity than nystatin or amphotericin B. Tests on the protection afforded by SPA-S-222 in Swiss albino mice infected with C, albicans were satisfactory as regards both the total protective dose and the partial protective dose (P.D. 50%).

Amphotericin B↗