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R Gagliardi

Publications and source records attributed to R Gagliardi.

At least 37 records · Page 2Linked to original sources
PubMed1989

Studies on heterocyclic compounds: 1,3-thiazolidin-4-one derivatives. III. Biological activity of halogenated 2,3-diaryl-1,3-thiazolidin-4-ones.

In previous communications from these laboratories, thiazolidinone derivatives of general formula (A) were synthesized and screened for antimicrobial activity. (formula; see text) where: X = H, CH3 Ar = phenyl Ar' = fluorinated or chlorinated phenyl The present communication is in part concerned with further extension of these studies to variously halogenated thiazolidinones of general formula (B). (formula; see text) where: X = H, CH3 R = H, 2-F, 3-F, 4-F, 3-Cl, 4-Cl R' = H, 4-F, 4-Cl These compounds were prepared by the general synthetic procedure previously reported for the 1,3-thiazolidin-4-one derivatives already prepared and screened in this SARs program. The general synthetic approach involves the cyclocondensation of the appropriate Schiff bases with alpha-mercaptoalkanoic acids such as thioglycolic and thiolactic acid. The prepared compounds were tested for their possible activity by a disk-diffusion assay (Kirby-Bauer modified). The organisms used were: S. aureus, S. beta-haemoliticus, B. subtilis, M. paratuberculosis 607, S. typhi, Kl. pneumoniae, E. coli Bb, Ps. aeruginosa, C. albicans, A. niger, S. cerevisiae. The results of this antimicrobial screening showed that the prepared compounds exhibited varying degrees of activity against Gram-positive, Gram-negative bacteria, and fungi. The second half of this report deals with the structure-activity relationships in all the compounds prepared and studied in this research program. For comparison of antimicrobial activity, the growth inhibitory activity of all the halogenated thiazolidinones of type (A) and (B), prepared and screened in this SARs study, were tabulated.(ABSTRACT TRUNCATED AT 250 WORDS)

Bacteria↗
PubMed1989

Studies on heterocyclic compounds: 1,3-thiazolidin-4-one derivatives. IV. Biological activity of variously substituted 2,3-diaryl-1,3-thiazolidin-4-ones.

The following 2,3-diaryl-1,3-thiazolidin-4-ones of general formula (A) were synthesized and screened for antimicrobial activity. (formula; see text) where: X = H (I, III, V, VII, IX, XI, XIII, XV, XVII, XIX, XXI, XXIII), CH3 (II, IV, VI, VIII, X, XII, XIV, XVI, XVIII, XX, XXII, XXIV); R = H (I, II, V, VI, VII, VIII, XI, XIII), 4-CH3 (XXI, XXII, XXIII, XXIV), 4-Br (III, IV, IX, X), 2-NO2 (XIII, XIV), 3-NO2 (XV, XVI), 4-NO2 (XVII, XVIII), 4-OCH3 (XIX, XX); R' = H (I, II, III, IV, XIII, XIV, XV, XVI, XVII, XVIII, XIX, XX, XXI, XXII), 4-CH3 (XXIII, XXIV), 3-Br (V, VI), 4-Br (VII, VIII, IX, X), 4-J (XI, XII). These compounds were prepared by the general synthetic procedure previously reported for the 1,3-thiazolidin-4-one derivatives already prepared and screened in this SARs program. The synthetic approach involves the cyclocondensation of the appropriate Schiff bases with alpha-mercaptoalkanoic acids. The prepared compounds were screened against S. aureus, S. beta-haemolititicus, B. subtilis, M. paratuberculosis 607, S. typhi, Kl. pneumoniae, E. coli Bb, Ps, aeruginosa, C. albicans, A. niger, S. cerevisiae by a disk-diffusion assay (Kirby-Bauer modified). The results obtained in this investigation showed that the prepared compounds exhibited varying degrees of antimicrobial activity. They were especially inhibitory toward Gram-positive bacteria, and fungi. 4-Nitroderivatives (XVII), (XVIII), and 2-nitroderivatives (XIV) and (XIII) possessed marked antimicrobial activity against S. aureus, S. beta-haemoliticus, and B. subtilis.(ABSTRACT TRUNCATED AT 250 WORDS)

Bacteria↗
PubMed1989

Structure-activity relationships of hydrazono derivatives of biological interest.

The following hydrazono derivatives (I-XXIII) of type (A), (formula; see text) where: X = NO2 (II, IV, VI, VIII, X, XIV-XXIII), X = H (I, III, V, VII, IX, XI, XII, XIII), and Y = H (I, II); 3-Cl (III, IV); 4-Cl (V, VI); 3,4-Cl2 (VII, VIII); 2,6-Cl2 (IX, X); 2-NO2 (XI); 3-NO2 (XII); 4-NO2 (XIII, XIV); 2-F (XV); 3-F (XVI); 4-F (XVII); 2-OH (XVIII); 4-OH (XIX); 2,4-(OH)2(XX); 2,4,6-(OH)3(XXI); 2,3-(OH,NO2) (XXII); 2,4-(NO2)2 (XXIII), were prepared and tested for antibacterial and antifungal activity. All of these compounds were prepared in satisfactory yield by reaction of aromatic aldehydes with 2-furoyl and 5-nitro-2-furoyl hydrazide. The hydrazono derivatives I-XXIII prepared in this investigation were screened for antimicrobial activity by a disk-diffusion assay (Kirby-Bauer modified). The organisms used were laboratory cultures of S. aureus, S. -haemoliticus, B. subtilis, M. paratuberculosis, E. coli, S. typhi, Ps. aeruginosa, K1. pneumoniae, A. niger, S. cerevisiae, C. albicans. The results of this study showed that a number of the prepared hydrazono derivatives exhibited varying degrees of activity against Gram-positive and Gram-negative bacteria. Compounds IV and XV possessed broad spectrum "in vitro" against Gram-positive and Gram-negative bacteria. Compounds XII greater than IV greater than XV showed inhibitory activity especially toward S. aureus. Compounds IV greater than XV greater than XVI were especially active against E. coli. Compounds XV greater than IV were especially inhibitory toward S. typhi and most of the prepared compounds inhibited considerably Ps. aeruginosa and K1. pneumoniae.

Anti-Bacterial Agents↗
PubMed1988

Efficacy and safety of ciprofloxacin in the treatment of UTIs and RTIs in patients affected by liver diseases.

The clinical efficacy and the safety of ciprofloxacin was studied in 92 patients (aged 26 to 83 years; mean 57.5 years) affected by urinary tract infections (UTI) and respiratory tract infections (RTI) suffering also with various liver diseases. Ciprofloxacin was given orally at different dose regimens: 500 mg b.i.d. (22 cases), 250 mg b.i.d. (20 cases), 500 mg s.i.d. (20 cases) for the treatment of UTIs; 500 mg b.i.d. (ten cases) and 250 mg b.i.d. (20 cases) for the treatment of RTIs. The doses were not correlated to the severity of the infections. Patients were treated for five to 15 days. All the bacteria isolated from sputum or urine before treatment were sensitive to ciprofloxacin (MIC range less than or equal to 0.015 mg/l to 8 mg/l). The clinical and bacteriological responses were favourable in a high percentage of patients both for RTIs and UTIs, irrespective of the dose. Side effects were infrequent (7%) and mild (nausea, gastralgia, oral candidosis), never requiring the interruption of the treatment. No change in the blood chemistry tests was observed at any dose.

Adult↗
PubMed1988

Incidence of stroke in young adults in Florence, Italy.

A population-based study specifically addressing stroke in young adults (aged 15-44 years) was conducted in Florence, Italy, from 1983 to 1985. We identified 47 cases of first stroke by means of a daily check of the medical facilities of the city and nearby towns and a review of death certificates. Patients were assessed by a neurologist shortly after the onset of the stroke, and computed tomography or autopsy was performed in 96%. The average annual incidence rate for all stroke (cases per 100,000 population per year) was 9.0 (95% confidence interval 5.8-13.4) for males and 8.7 (95% confidence interval 5.5-13.0) for females. The average annual incidence rates for the pathologic types of stroke were 3.4 for cerebral infarction, 3.2 for subarachnoid hemorrhage, and 1.9 for intracerebral hemorrhage. The case-fatality ratio was 23.4% at 1 month. Among patients with ischemic strokes, atherosclerosis and cardiac disease accounted for 50% of the cases. Based on angiography or autopsy findings, aneurysm or arteriovenous malformation were demonstrated in 88% of the patients with subarachnoid hemorrhage. In 50% of the patients with intracerebral hemorrhage, no cause of bleeding was detected. Our study may supply information about stroke pathologic types in an unselected series of young adults.

Adolescent↗
PubMed1987

Efficacy and safety of oral ciprofloxacin in the treatment of respiratory tract infections associated with chronic hepatitis.

Twenty patients with lower respiratory tract infections presumably caused by ciprofloxacin-susceptible bacteria were admitted to a non-comparative, prospective clinical study. All patients were hospitalized for chronic hepatitis at various stages of the disease. Ciprofloxacin was given orally at a dose of 250 mg every 12 hours for five to 10 days. Patients had either acute bronchitis, chronic bronchitis in the acute phase, or acute tracheobronchitis. In 19 of 20 patients treated, there was a favorable outcome (15 cures and four improvements). In 17 patients, the presumably causative pathogen was eradicated. No side effect was observed except for oral candidiasis, which occurred in two patients. This study demonstrates the clinical and bacteriologic efficacy of ciprofloxacin in pulmonary infection in patients with severe impairment of liver function.

Administration, Oral↗
PubMed1987

Metabolic effects of long-term therapy with muzolimine and chlorthalidone in hypertension.

Previous short-term studies of muzolimine (a diuretic with frusemide-like activity) had shown that it did not induce a significant change in the serum potassium concentration. In the present study sodium and potassium handling and other metabolic variables have been compared during 16 weeks of therapy with muzolimine and chlorthalidone, a thiazide-like diuretic. During muzolimine treatment, plasma and red cell potassium concentrations remained unchanged, while a significant fall in potassium occurred with chlorthalidone. Neither drug affected the activity of sodium-potassium cotransport or sodium-lithium countertransport in red cells in vitro. Muzolimine and chlorthalidone had similar effects on arterial pressure and on the other metabolic variables tested.

Adult↗
PubMed1986

[Bacterial lysis by lysozyme].

We confirmed the previous reports of Fleming, Nakamura et al. on the inability of lysozyme to lyse Micrococcus lysodeikticus cells at an acidic pH (3.0 - 3.5). In these conditions, lysozyme binds to the mucopolysaccharides of the cell wall without showing any lytic activity; lysis occurs at very high rate when pH is raised at neutral values by adding alkaline solutions. Our results were obtained by monitoring bacterial cultures both in aqueous solutions and on agar plates.

Animals↗
PubMed1985

Cross-over study of muzolimine and hydrochlorothiazide-amiloride in hypertensive patients.

Thiazide therapy is a widely used first line treatment for arterial hypertension. Its useful value, particularly in mild or moderate hypertension, is sometimes reduced by metabolic side-effects, as hypokalaemia and hyperuricaemia. In the present study the antihypertensive efficacy of a new, non-sulphonamide diuretic Bay g 2821 (muzolimine) was evaluated in comparison with the combination of hydrochlorothiazide-amiloride over a period of 4 weeks. A highly significant decrease in systolic and diastolic blood pressures was produced by both treatments. No decrease in serum potassium nor an increase in cholesterol, triglycerides, uric acid or glucose was detected during the 4 week treatment period. Subjective side-effects, such as headache and dizziness, were very rarely observed during Bay g 2821 treatment. The new diuretic appears, therefore, to be effective in the treatment of arterial hypertension without untoward side-effects.

Adult↗
PubMed1985

Antihypertensive and cardiovascular effects of nitrendipine: a controlled study vs. placebo.

The antihypertensive and cardiovascular effects of nitrendipine, a calcium entry blocker similar to nifedipine, have been evaluated in a double-blind, placebo-controlled study in 20 patients with hypertension. At baseline and at the end of the 8-week period (nitrendipine, 20 mg once a day, or placebo, 1 tablet once a day) the following parameters were measured: systolic and diastolic blood pressure (BP) and heart rate (HR) at rest by an automatic recorder; BP, HR, and cardiac workload (systolic BP X HR) during exercise testing on a bicycle; left ventricular mass (LVMe according to the method of Devereux) and cross-sectional area (CSA), and main parameters of systolic function (end diastolic volume, end systolic volume [ESV], and ejection fraction [EF]) by M mode echocardiography. There was a significant decrease in BP at rest (163/108 vs. 144/92 mm Hg; P less than 0.001) and during exercise in subjects receiving nitrendipine, while placebo did not modify these parameters. LVMe (from 195 to 188 gm; P less than 0.01) and CSA (from 20.2 to 19.8 cm2; P less than 0.05) were reduced by nitrendipine, which also improved cardiac performance (ESV fell from 44 to 38 ml [P less than 0.001] and EF fell from 62% to 66% [P less than 0.01]). No effect was observed in the placebo group. Our results indicate that nitrendipine is a powerful antihypertensive agent that also improves cardiac performance and slightly but significantly reduces left ventricular mass.

Administration, Oral↗
PubMed1984

Extra-intracranial arterial bypass in typical carotid reversible ischaemic deficits: long-term follow-up in 100 patients.

The long-term follow-up of 100 consecutive patients who suffered from a reversible ischaemic attack (RIA) in the carotid territory and were submitted to extra-intracranial arterial bypass (EIAB) surgery in seven Italian Neurosurgical Centres is reported. The preoperative angiographic and clinical features, and the surgical complications are reported. The follow-up ranged from two to seven years with a mean of thirty-five months. In this period in the territory served by the bypass only two completed strokes and six RIAs occurred. Four patients died, only one for cerebral ischaemic problems. The results of the present series have been compared with those of the literature: they appeared consistent with other surgical series and clearly better than those of medical treated patients. The EIAB can then be considered a good therapeutic choice for the treatment of RIAs in carotid territory.

Adult↗
PubMed1984

Long-term follow-up in 257 ICA occlusion: comparison between EIAB-treated and untreated patients.

The purpose of this paper is to estimate the real value of the Extra-Intracranial Arterial Bypass (EIAB) in preventing or reducing further and more catastrophic ischaemic events in patients suffering from an Internal Carotid Artery (ICA) occlusion. 257 patients, suffering from ICA occlusion, are considered retrospectively: 122 of them submitted to EIAB and 135 medically treated or untreated. In both groups, homogeneous by sex, age, neurological grading distribution and length of follow-up, the following parameters were considered: the incidence of ischaemic recurrences during the follow-up period; the characters of the recurrences with particular reference to the fatal stroke; the rate of ischaemic events per year. The comparison between the outcome in surgically treated patients and in "untreated" ones indicates that the EIAB can be effective in preventing or reducing the ischaemic recurrences and the frequency of fatal stroke in TIA-, RIND, or stroke-patients suffering from ICA occlusion.

Adult↗