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Biomedical subjects

R Giorgi

Publications and source records attributed to R Giorgi.

At least 73 records · Page 4Linked to original sources
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

Effects of maternal exposure to polychlorobiphenyls (PCBs) on F1 generation behavior in the rat.

The effect of Fenclor 42 (PCB) exposure of female rats (Fischer 344 strain) was studied through assessment of the behavioral development of their F1 progeny. Female rats were exposed to PCB according to the following treatment schedule: (A) (5 days) 2 weeks prior to mating, (B) during gestation (Days 6-15 of pregnancy), (C) during lactation (Days 1-21 after delivery). Behavioral endpoints of motor reflexes, motor coordination, activity (preweaning behaviors), and learning (postweaning behavior) were evaluated for PCB ip dosages of 5-10 mg/kg/day for 5 days (preconception exposure), and PCB oral dosages of 2-4 mg/kg/day for 10 days (in utero exposure) and of 1-2 mg/kg/day for 20 days (during lactation exposure). Dosage-dependent differences in the evaluated behaviors were found in the offspring of the PCB-exposed females when compared to the offspring of corn-oil (vehicle)-exposed females. Significant differences in the development of cliff avoidance reflexive behavior, swimming ability, and open field activity were particularly evident. Furthermore the PCB exposure of female rats during gestation and lactation resulted in impaired acquisition of the active avoidance behavior while preconceptional PCB exposure significantly affected active avoidance performance as reflected in increased number of avoidance responses to reach criterion for extinction. These results show that Fenclor 42 does possess a significant risk to the offspring of exposed females, and further illustrate the sensitivity of progeny behavioral assessment in detecting suspected functional teratogenesis.

Aging↗
PubMed1988

Synthesis and cognition activating properties of some mono- and bicyclic lactam derivatives.

Upon reductive cyclization cyano esters 2, 3, and 9 yielded piperidones and perhydropyrrolo[3,4-c]pyridine lactams, generally as a mixture of diasteromeric cis-trans forms. X-ray crystallographic analyses were carried out on bicyclic dilactam derivatives 6 and 10, and a cis configuration at the ring junction was determined in both cases. A series of neuropsychopharmacological tests performed on the title compounds indicated that they are generally nontoxic even at high doses (up to 1000 mg/kg ip). The cognition activating properties of lactams 4, 5, 6, and 10 were evaluated in enhancing retention for passive avoidance learning in rats without and after electroconvulsive shock (ECS); compounds 5 and 10 were found to be more potent than piracetam in the amnesia-reversal testing.

Amnesia↗
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

Complementation studies in cells from patients affected by trichothiodystrophy with normal or enhanced UV photosensitivity.

A normal level of UV-induced DNA-repair synthesis (UDS) was observed in fibroblasts from a patient affected by trichothiodystrophy (TTD) without photosensitivity. This finding indicates that the hypersensitivity to UV light and the reduced UDS due to the presence of xeroderma pigmentosum complementation group D mutation (XP-D), described in photosensitive TTD patients, are not constantly associated with TTD. Complementation analysis in heterokaryons, obtained by fusion of repair-proficient with repair-deficient TTD cells, demonstrates that cells from the patient showing normal photosensitivity are able to restore UDS in UV-hypersensitive TTD cells.

Cell Fusion↗
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

[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

Chromosomal effects of methotrexate on cultured human lymphocytes.

The effect of MTX on chromosome morphology was analyzed in cultured lymphocytes, and a high percentage of aberrant mitoses was found. Chromosome anomalies, such as gaps and breaks, are observed on all the chromosomes, but are preferentially located on chromosome n.3 at band p14. When the cells were continuously exposed to the drug, the chromosome damage appeared to be particularly severe.

Cells, Cultured↗
PubMed1983

Cephalosporins. VI. Synthesis and structure-activity relationships of new 7 beta-[(Z)-2-alkoxyimino-2-(2-aminothiazol-4-yl)acetamido]cephalosporins with a tetraxolopyridazine at the 3-position.

The synthesis and in vitro activity of 7 beta-[(Z)-2-alkoxyimino- 2-(2-aminothiazol-4-yl) acetamido]cephalosporins with a tetrazolo[1,5-b]pyridazine at the 3-position are described. These cephalosporins showed excellent activity against Gram-negative bacteria, including beta-lactamase producing strains. The most interesting compound of the series was 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyimino acetamido] -3-(8-carboxytetrazolo[1,5-b]pyridazin-6-yl)- thiomethyl-3-cephem-4-carboxylic acid (9, FCE 20485) because of its extraordinarily long half-life and marked in vivo activity.

Cephalosporins↗
PubMed1980

Frequencies of sister-chromatid exchanges in relation to cell kinetics in lymphocyte cultures.

The frequency of sister-chromatid exchanges (SCE) was determined on second-division metaphases of lymphocytes stimulated by phytohaemagglutinin (PHA) during 9 days of culture. By using either a continuous or a pulsed bromodeoxyuridine (BUdR) treatment, cells were selected that had divided only twice, or at least twice, after different culture periods. No significant differences were observed in the SCE frequencies among the various samples. The incidence of SCE appears to be independent of the proliferation properties of cultured lymphocytes, such as length of cell cycle, fast or delayed response to PHA and number of divisions performed in vitro.

Adult↗
PubMed1976

Incorporation of (3H)thymidine stimulated by ultraviolet radiation into human fibroblast cultures.

We studied DNA repair synthesis after ultraviolet irradiation in human fibroblasts cultured in vitro by measuring the ultraviolet-stimulated incorporation of [3H]thymidine into cells in which the semi-conservative DNA replication was inhibited by hydroxyurea. Experiments performed with five fibroblasts lines derived from healthy donors showed a relatively fast initial process ( that is completed within 1 h for 100 erg/mm2 and within 2 h for 500 erg/mm2) and a subsequent slower process, evident between 2 and 6 h after irradiation. The repair capacity of normal cells is expressed by the difference between the values of incorporation (in presence of hydroxyurea) of irradiated and control cells. The pattern of repair was similar in all five cell lines: repair capacity was positive and the amount of repair synthesis increased with incubation time after UV irratiation. Similar experiments were performed with fibroblasts derived from five patients with the classical xeroderma pigmentosum (XP) and from one patient with the De Sanctis-Cacchione syndrome. Normal and XP cells could be distinguished according to whether they displayed a positive or negative value of repair synthesis and/or according to the degree of the slope of the repair synthesis curve as a function of the incubation time after irradiation. We conclude that the technique used in our experiments can demonstrate in a rapid and simple way a defect in the repair capacity in fibroblast cultures; the data are in good agreement with those obtained in the same XP cell lines by other authors [9], who have measured unscheduled DNA synthesis in autoradiographs and repair replication after addition of BUdR.

Cells, Cultured↗