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Biomedical subjects

S Massa

Publications and source records attributed to S Massa.

At least 109 records · Page 6Linked to original sources
PubMed1987

[Antibacterial and antifungal compounds. VIII. Synthesis and antifungal activity of pyrrol derivatives similar to trichostatin A].

Some p-methylbenzolpyrrole acrylic acids and related compounds were synthesized. The new pyrrole derivatives have structural features in common with trichostatin A, an antifungal antibiotic. The above acids and derivatives were tested against Candida albicans and Candida sp in comparison with miconazole, pyrrolnitrin and amphotericin B and showed very weak antifungal activities. Occasionally some activity was found against a few strains of Candida albicans and against Candida pseudotropicalis.

Antifungal Agents↗
PubMed1987

Potential antitumor agents. II. Lappin intramolecular cyclization of diethyl 3-carbazolylaminomethylenemalonate: a structure assignment.

Diethyl 3-carbazolylaminomethylenemalonate undergoes Lappin cyclization giving 2-carbethoxy-1-oxo-1,4-dihydro-7H-pyrido[2,3-c]carbazole. Formation of an angular pyridocarbazole derivative is consistent with the Markwald rule. The synthesis of 4-ethyl derivatives of the above pyridocarbazole and its 8,9,10,11-tetrahydro derivative is also reported as a goal to potential indoloquinolone antitumoral agents.

Antineoplastic Agents↗
PubMed1986

[Antibacterial and antifungal agents. VI. Pirfloxacin and related compounds: synthetic and microbiological studies].

A new route to pirfloxacin, a fluorinated pyrrylquinolone with high broad-spectrum antibacterial activities, is described starting from 7-amino-1-ethyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid and 2,5-dimethoxytetrahydrofuran. When the reaction with the latter compound was carried out using the ethyl ester of the above acid the related pyrryl ester formed, which on alkaline hydrolysis gave pirfloxacin. The synthesis and antibacterial activities of the 1-allyl analogue of pirfloxacin and of 7-[2-(1-pyrrolidinomethyl)-1-pyrryl]-1-ethyl-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid and its 6-fluoroderivative are also reported.

Anti-Bacterial Agents↗
PubMed1986

[Non-steroidal anti-inflammatory agents. IV. Synthesis and pharmacologic activity of aroylthiopheneacetic acids with a pyrrole group].

The synthesis of new antiinflammatory aroylthiopheneacetic acids bearing a pyrrole moiety is described. These compounds can be regarded as analogues of thiaprofen and related isosteres. The antiinflammatory activity of the new pyrryl derivatives has been evaluated in comparison with indomethacin, tolmetin and the unknown 5-(2-chlorobenzoyl)thiophene-2-acetic acid. Among tested derivatives the compounds containing the pyrrole ring were devoid of analgesic-antiinflammatory activities.

Animals↗
PubMed1985

1-Ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1H-pyrrol-1-yl)-quinoline-3-carb oxylic acid, a new fluorinated compounds of oxacin family with high broad-spectrum antibacterial activities.

The synthesis of 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1H-pyrrol-1-yl)quinoline-3-carboxy lic acid, a new fluorinated high broad-spectrum antibacterial agent related to nalidixic acid is described. The title compound has been prepared by the reaction of 4-fluoro-3-(1H-pyrrol-1-yl)aniline with diethyl ethoxymethylenemalonate, cyclization of the malonate obtained to the quinolinecarboxylate ester, ethylation of the ester, followed by hydrolysis with aqueous sodium hydroxide. The new derivative proved very active against both gram-positive and gram-negative bacteria. Its activities in comparison with those of nalidixic acid, pipemidic acid, piromidic acid and enoxacin were found to be greatly superior with regard to the unfluorinated compounds and somewhat superior also to enoxacin. The known 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(pyrrolidin-1-yl)quinoline-3- carboxylic acid, here prepared by catalytic hydrogenation of the pyrrole moiety of the title compound, has been found to be less active as an antibacterial agent.

Anti-Bacterial Agents↗
PubMed1985

[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↗
PubMed1985

[New psychotropic agents. 2. Synthesis and pharmacologic activity of derivatives of 5H-pyrrolo[1,2-b][1,2,5]benzotriazepines].

Bischler-Napieralski intramolecular cyclization of N-(2-aroylaminophenyl)-N-methyl-1H-pyrrol-1-amines and reaction of arylaldehydes on N-(2-aminophenyl)-N-methyl-1H-pyrrol-1-amine furnished 11-aryl-5-methyl-5H-pyrrolo[1,2-b][1,2,5]benzotriazepines and 11-aryl-10,11-dihydro-5-methyl-5H-pyrrolo[1,2-b][1,2,5]benzotriazepin es respectively. The latter reaction required in some cases the use of p-toluenesulphonic acid as a catalyst. The new tricyclic derivatives described were tested for pharmacological evaluation of their psychotropic activity.

Animals↗
PubMed1984

Typical and reverse bobbing: a case with localizing value.

Report of a case of typical bobbing occasionally interpolated by reverse bobbing. The causative lesion, which lay in the most dorsal median portion of the pontine tegmentum, was a small primary hemorrhage, diagnosed in life by CT scanning and confirmed at necropsy. The pathological and clinical correlations of the phenomenon are discussed.

Aged↗
PubMed1984

[Non-steroidal anti-inflammatory agents. III. Synthesis and analgesic-anti-inflammatory activity of 4-(pyrrol-1-yl)phenylacetamides and 4-(pyrrol-1-yl)phenethylamines].

Preparation of some 4-(pyrrol-1-yl)phenylacetamides and 4-(pyrrol-1-yl)phenylethylamines starting from 4-(pyrrol-1-yl)phenylacetic acid is reported. The new compounds were tested as analgesic-antiinflammatory agents. Data from pharmacological screening indicate 1-[4-(pyrrol-1-yl)phenylethyl]piperidine as the most active substance.

Acetamides↗
PubMed1984

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↗
PubMed1984

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↗
PubMed1984

[Palpebral nystagmus].

A case of palpebral nystagmus is reported. Two infarcts were present in the rostral pons, caudal midbrain and in the periaqueductal gray matter between the red nuclei, ventrally to the posterior commissure. The relationships between the palpebral nystagmus and the retraction of the upper lid together with the clinico-pathological significance of the two signs is discussed.

Brain Stem↗