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Biomedical subjects

I Giorgi

Publications and source records attributed to I Giorgi.

At least 19 recordsLinked to original sources
PubMed2002

Functional and psychological recovery during intensive hospital rehabilitation following cardiac surgery in the elderly.

UNLABELLED: The recovery process in the elderly after cardiac surgery is influenced not only by clinical cardiac conditions, but also by comorbidity, cognitive decline and disability. We evaluated the relationship between clinical objective and self-perceived factors and their influence on functional recovery in 204 consecutive, over-70s pts who were admitted into an intensive hospital rehabilitation program following cardiac surgery. The variables taken into consideration were: comorbidity (Charlson index), length of hospital stay and complications in cardiac surgery and rehabilitation, disability (nursing needs score index), functional status (6-min walking test), left ventricular EF, number of training sessions, self-perceived health status (EuroQol questionnaire), emotional impairment (anxiety/depression, CBA-2.0/interview). RESULTS: Functional capacity: the distance walked was 198 +/- 103 m at admission and 287 +/- 121 m at discharge (p < 0.0001). Only the nursing needs score index resulted as a weak, independent predictor of the distance walked at admission (r2 = 0.14, p < 0.001, beta = 0-.21), which (beta = 0.49), together with complications during rehabilitation (beta = -0.15), self-perceived health status at discharge (beta = 0.15) and number of training sessions (beta = 0.20), was independently correlated with the distance walked at time of discharge (r2 = 050, p < 0.0001). Patients mood: anxiety correlated with depression. Emotional scores did not correlate with functional measures. Patients self-perceived health status: only the nursing needs score index was a weak, independent predictor of well-being at entry (r2 = 0.15, p < 0.0001, beta = -0.29), which, in turn, was the only predictor of perception at discharge (r2 = 0.33, p < 0.0001, beta = 0-.42). CONCLUSIONS: In an intensive hospital rehabilitation program following cardiac surgery in patients over 70 a) there was no correlation between clinical and psychological variables; b) anxiety and depression were associated, but neither influenced the recovery process nor correlated to health status perception; c) functional impairment was strongly influenced by nursing needs which also affected the self-perceived health status; d) both functional and perception recovery were influenced by disability at time of admission and reacted positively after rehabilitation.

Age Factors↗
PubMed2001

New 5-substituted-1-(2-hydroxybenzoyl)-benzotriazoles, potassium channel activators. IV.

This paper reports the synthesis of a series of new 5-substituted-1-(2-hydroxybenzoyl)-benzotriazoles, which have been tested for their activity as possible activators of potassium channels. In rat aortic rings, the 'opened' derivatives 1a-f, intermediates of synthesis, showed vasorelaxing properties, with appreciable values of potency. However, the most remarkable effects were recorded for the 2-hydroxybenzoylbenzotriazoles 3a-f, which showed full vasorelaxing efficacy and high potency values. The introduction of a 2-hydroxybenzyl substituent in the 1 position of the benzotriazole ring (compound 7) strongly decreased the activity, showing the importance of the electron-acceptor carbonyl function. The best compound, 3b, was further investigated, in order to evaluate the possible mechanism of action involved in the vasodilator activity. In the vascular model, different potassium channel blockers inhibited the effects of the compound, and an increase of the levels of membrane depolarisation induced a significant reduction of the recorded responses. Compound 3b was also tested in a model of isolated rat heart, retroperfused through the aorta and submitted to a global ischemia/reperfusion cycle. In such an experimental condition, 3b showed an interesting cardioprotective activity. All the above observations are in agreement with the hypothesis of a mechanism linked to the activation of potassium channels.

Animals↗
PubMed2001

Some structural changes on triazolyl-benzotriazoles and triazolyl-benzimidazolones as potential potassium channel activators. III.

This paper reports the synthesis and pharmacological evaluation of some compounds, obtained by structural modifications of 1,2,3-triazolyl-benzotriazoles and 1,2,3-triazolyl-benzimidazolones, which had shown activity as potential activators of the big-conductance calcium-activated potassium channels (BK(Ca)). Changes have concerned the introduction of a hinderer substituent in the 5-position of the benzimidazolone (4a, b) and benzotriazole (5a, b) rings, opening of the benzimidazolone ring (7) and substitution of the 1,2,3-triazole ring with a 2-hydroxyphenyl ring (10). Furthermore a series of 3-aryl-benzotriazin-4-one derivatives (13a-e) has been studied, which appears as a modification and/or combination of the benzimidazolone and benzotriazole rings. Only compound 10 shows interesting activity, while the other structural modifications either do not increase (compounds 4 and 5) or reduce (compounds 7 and 13) the pharmacological activity. However, these results provide useful information about structure-activity relationships.

Animals↗
PubMed2001

2-Alkyloxyalkylthiohypoxanthines as new potent inhibitors of xanthine oxidase.

The title compounds were prepared and tested as xanthine oxidase (XO) inhibitors. Results evidenced that potency was related to the position of the oxygen atom in the 2-linear chain and that it grew with distance from the sulfur atom until it became equipotent to 2-n-hexylthiohypoxanthine. Enzymatic oxidation on C(2) occurred in the 8-alkylthiohypoxanthines. On the contrary, oxidation on C(8) did not occur in the 2-alkythioderivatives, demonstrating that the chain forced these molecules to form a complex with molybdenum(VI) involving only the N(3) and N(9) nitrogen atoms.

Enzyme Inhibitors↗
PubMed2001

New 2-(2'-phenyl-9'-benzyl-8'-azapurin-6'-ylamino)-carboxylic acid methylesters as ligands for A1 adenosine receptors.

Synthesis of a series of new 2-phenyl-9-benzyl-8-azaadenines bearing on N6 an alkyl or aralkyl chain having a carbonyloxymethyl group on the carbon bound to N6 were reported. The ester group could assure to the molecule a better water-solubility than the 8-azaadenines 2, 6 and 9 substituted with lipophilic groups synthesised in the past. Compounds synthesised demonstrated only little capability of binding A1 adenosine receptors.

Adenine↗
PubMed2000

Triazolyl-benzimidazolones and triazolyl-benzotriazoles: new potential potassium channel activators. II.

This paper reports the synthesis and pharmacological evaluation of a series of 5-substituted-triazolyl benzotriazoles (2a-f) and the corresponding series of 5-substituted-triazolyl-benzimidazolones (6a-f), as potential activators of the big-conductance calcium-activated potassium channels (BK(Ca)). The synthesis and structure demonstration of the stock compounds of the two series have been described in our previous works, as well as the common starting compounds 4-carboxamido-5-(4-substituted-2amino-anilino)-1,2,3-triazoles (1a-f). The triazolyl-benzotriazoles were obtained by diazotization, while the triazolyl-benzimidazolones were obtained by thermal intramolecular cyclization of ethoxycarbonylamino derivatives or directly with phosgene. Benzimidazolone compounds generally showed little effect whilst the compounds with a benzotriazole ring showed full efficacy, with vasorelaxing properties and potency parameters a little lower than that of the reference compound NS 1619. These effects were significantly reduced by an increased membrane depolarization. This depolarization-sensitive response is in agreement with the pharmacodynamic hypothesis of activation of potassium channels.

Animals↗
PubMed2000

Substituted 1,2,3-triazolo[1,5-a]quinazolines: synthesis and binding to benzodiazepine and adenosine receptors.

This paper reports the synthesis and evaluation of the biological affinity towards benzodiazepine and A(1) and A(2A) adenosine receptors of some 3-ethoxycarbonyl or 3-phenyl-substituted 1,2, 3-triazolo[1,5-a]quinazolines. Starting from the appropriate chloro-substituted phenylazides, the series of 7 or 8 chloro-substituted triazoloquinazolines were prepared. Nitration reactions of the triazoloquinazoline ring and chlorination reactions of the hydroxyl group in the 5 position of the same ring are also reported. By nucleophilic displacement of halogen, the corresponding 5-amino derivatives and some analogous derivatives bearing cyclohexylamino and p-toluidino substituents were obtained. The binding assays showed a generalized decrease in the affinity towards the benzodiazepine receptors and confirmed a moderate affinity towards the A(1) adenosine receptors in comparison with the previously studied triazoloquinazoline derivatives.

Animals↗
PubMed1999

Lesson learnt from a halt of the hospital information system.

The present paper deals with an experience of blackout of the hospital information system at our Medical Centre, trying to evaluate the impact on internal users (physicians, nurses, clerks) and patients population. Limited inconveniences have occurred to out-patients in terms of delay in collecting medical reports after diagnostic test execution. As regards direct users, impact was evaluated through a structured interview. Administrative personnel, that have been using computer-based system for at least ten years, have not declared particular inconveniences, accepting the overtime or the extra-work as simply unavoidable. On the contrary, health-care personnel reported a heavy negative impact of the system failure on their activity. After a great effort to achieve the system acceptance and direct physicians usage, the blackout of the system has pointed out that the situation has changed since a few years ago: now the HIS, and particularly its clinical core, is considered mission critical.

Data Collection↗
PubMed1998

Novel 3-aralkyl-7-(amino-substituted)-1,2,3-triazolo[4,5-d]pyrimidines with high affinity toward A1 adenosine receptors.

Three series of several 1,2,3-triazolo[4,5-d]pyrimidine derivatives bearing various amino substituents at the 7 position and one of three lipophilic substituents at the 3 position (benzyl, phenethyl, or 2-chlorobenzyl) were prepared starting from the corresponding 7-chloro compounds, by nucleophilic substitution by the appropriate amine. Radioligand binding assays at bovine brain adenosine A1 and A2A receptors showed that some compounds possessed a high affinity and selectivity for the A1 receptor subtype. In particular the biological results suggested the compounds bearing cycloalkylamino (cyclopentyl- and cyclohexylamino) or aralkylamino (alpha-methylbenzyl- and 1-methyl-2-phenylethylamino or amphetamino) substituents at the 7 position were the most active derivatives. The best lipophilic substituent at the 3 position was the 2-chlorobenzyl (A1 affinity Ki < 50 nM) followed by the benzyl and then the phenethyl groups. This pattern of structure-activity relationship (SAR) was similar to that previously reported for analogous 1,2,3-triazolopyridazino derivatives (Biagi et al., 1994, 1995, 1996) except for the compounds bearing substituted aromatic amines which presented a generalized and strong decrease of the A1 receptor affinity. These facts allowed us to attribute to these molecules a binding mode within the A1 adenosine receptor analogous to that of the corresponding triazolopyridazines.

Adenosine↗
PubMed1998

1,2,3-Triazolo[1,5-a][1,4]- and 1,2,3-triazolo[1,5-a]-[1,5]benzodiazepine derivatives: synthesis and benzodiazepine receptor binding.

This paper reports the synthesis of new 1,2,3-triazolo[1,4]benzodiazepine and 1,2,3-triazolo[1,5]benzodiazepine derivatives and their evaluation toward benzodiazepine receptors. Receptor affinity gradually and remarkably increases by moving the nitrogen atom of the central ring from position 3 through 4 to position 5, to give the most effective compound 6a (Ki = 150 nM). N-methylation of the diazepine ring (7a) lowers receptorial binding. Introduction of a chlorine atom on the benzene ring doubles the Ki value (6b) which remains unaltered by the N-methylation (7b).

Animals↗
PubMed1998

A 3D model of the human A1 adenosine receptor. An evaluation of the binding free-energy with ligands.

A model of A1 adenosine receptor was built on the basis of the prediction of transmembrane helices made by PHDtopology and forcing the rough initial model over the scaffold of the rhodopsin. Only helices were accurately modeled. Several complexes between the model of the A1 receptor and some ligands were built. The binding site was hypothesized on the basis of biochemical experiments (site directed mutagenesis). Ligands were selected so that their Kis range between millimolar to nanomolar. The validation of the model was carried out performing calculations of the binding free energy between ligands and the receptor model. The free energy calculations were accomplished by using the linear free energy approximation method (LIE). We could observe that the trend of the calculated delta delta Gs (differences in binding free energies between the antagonist 2, showing the lowest Ki, and the other antagonists analyzed) agreed with the one obtained from biological data.

Adenosine↗
PubMed1998

New 1,2,3-triazole derivatives (ureas, amides, urethanes) with a potential biological interest.

This paper reports the preparation of three series of 1,2,3-triazole derivatives bearing an ureido substituent (compounds 5a-h), a carboxamido substituent (compounds 6a-f) or an urethane substituent (compounds 7a-l). Some compounds were submitted to in vitro functional tests on guinea-pig isolated intestinal preparations and/or to in vitro antitumor and antiviral screening. The tested compounds showed no activity on guinea-pig ileum, except compound 7g, provided of contracturant properties; similarly, no anticancer or antiviral significant activity was found.

Animals↗
PubMed1997

Spreading the clinical information system: which users are satisfied?

The present study deals with the assessment of the perceived usefulness and perceived ease of use of the clinical core of the HIS we are building, and progressively spreading into the medical centre, through the use of two questionnaires. The differences in subjective perception among clinical units and professional roles have been analyzed. Results show that the system, in use on a mandatory basis, has been accepted. Most of the users are satisfied, and probable removable causes of dissatisfaction have been identified.

Adult↗
PubMed1997

Synthesis of 4,6-disubstituted- and 4,5,6-trisubstituted-2-phenyl-pyrimidines and their affinity towards A1 adenosine receptors.

Synthesis and assay of title compounds are reported. The results can support our hypothesis about the possibility that molecules characterized by great flexibility, as the title 2-phenyl-4,5,6-triaminopyrimidines, can better interact with the receptor sites compared with rigid molecules as 2,6,9-trisubstituted 8-azaadenines. Relatively low activity shown by pyrimidine derivatives demonstrated the importance of the bicyclic aromatic system in 8-azaadenines and adenines to give a favourable interaction between a hexogenous molecule and the A1 adenosine receptors.

Animals↗
PubMed1996

Synthesis and biological evaluation of new imidazole, pyrimidine, and purine derivatives and analogs as inhibitors of xanthine oxidase.

Several derivatives of 4,5-disubstituted imidazole, 2,4,5-trisubstituted pyrimidine, 2-substituted purine, thiazolo[3,2-alpha]purine, [1,3]thiazino[3,2-alpha]purine, thiazolo[2,3-i]purine, [1,3]thiazino-[2,3-i]purine, and 6-substituted pyrazolo[3,4-d]pyrimidine were synthesized and tested as inhibitors of the xanthine oxidase enzyme. Of those, some 4-(acylamino)-5-carbamoylimidazoles and 2-thioalkyl-substituted purines exhibited very good inhibitory activity, being at least 500 times more effective than allopurinol. The ineffectiveness of 6-n-alkylpyrazolo[3,4-d]pyrimidines is imputable to the alkyl chain which could hinder the coordination with molybdenum according to the known mechanism for the binding of the inhibitor allopurinol; the effectiveness of imidazole derivatives, by contrast with the ineffectiveness of 4,5-diamino-2-(thioalkyl)-6-hydroxypyrimidines, indicates the relative importance of the five-membered ring in the interaction with the enzyme. Moreover, the marked effectiveness of the angularly-cyclized [1,3]thiazino[2,3-i]purinones, which constitute an interesting new class of inhibitors, together with the weak activity of linearly-cyclized derivatives, allowed us to characterize more precisely the lipophilic region of the enzyme facing the N(1)-C(2) positions of the substrate hypoxanthine.

Allopurinol↗
PubMed1996

1,2,3-triazolo[1.5-a]quinazolines: synthesis, benzodiazepine receptor binding and theoretical calculations.

This paper reports the synthesis of 3-substituted-1,2,3-triazolo[1,5-a]quinazolin-5-ones prepared by 1,3-dipolar cycloaddition reaction of 2-azidobenzoic acid to methylenic compounds activated by a cyano group. The new derivatives were submitted to benzodiazepine receptor binding assays: the results indicated an interesting receptorial affinity of the 1,2,3-triazolo[1,5-a]quinazoline ring. On the basis of the biological results, theoretical calculations were performed, which suggested useful structural modifications.

Animals↗
PubMed1996

Assessing users' satisfaction through perception of usefulness and ease of use in the daily interaction with a hospital information system.

The present study deals with the assessment of the subjective perception of the clinical core of the hospital information system (HIS) we are building. This HIS is not in use on a voluntary basis, but physicians and nurses use it for all the aspects of their inpatient care that have been informatized. Two questionnaires, aimed at the assessment of users perceived usefulness and ease of use of information technology, were utilized to: obtain feedback of the actual users' satisfaction as a predictive factor for the future life of the system, assess the real influence of the often-mentioned problems of age and unfamiliarity with computers of potential users, learn about the aspects which would enhance users' acceptance. The analysis of answers to the questionnaires has indicated a substantially positive perception of the system in terms of both usefulness and ease of use. This constitutes a good reason to keep on investing in the project. Even though this study has the intrinsic limit of the small dimension of the inquired population (53 users, equivalent to 98% of the personnel of the assessed clinical units), our data confirm the inconsistency of the relationship between perception of usefulness and age, and show "unfamiliarity with computers" as commonplace. On the other hand, it seems that the keystone for usefulness perception is the knowledge the users have of the system. An effort by the technical personnel in establishing a broader collaboration with the users, and in providing more exhaustive training and support may well be worthwhile.

Age Factors↗