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Biomedical subjects

R Silvestri

Publications and source records attributed to R Silvestri.

At least 37 records · Page 2Linked to original sources
PubMed1994

Non-steroidal antiinflammatory agents. Synthesis and enzyme inhibition of 2-[4-(heteroarylmethyl)phenyl] propanoic acids and analogues.

Some 2-[4-(heteroarylmethyl)phenyl]propanoic acids and phenylacetic and benzoic analogues has been synthesized. All above acids were tested for their inhibitory activity on lipoxygenase and cyclooxygenase, in comparison with NDGA and tolmetin. 2-[4-(Thien-2-ylmethyl)phenyl]propanoic acid 2, strictly related with suprofen, was found the most interesting compound, giving rise to a 79% inhibition of the cyclooxygenase activity at 10(-4) M concentration.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed1993

[Abrupt shift to zolpidem, a new imidazopyridine hypnotic, in insomniac patients previously treated with benzodiazepine hypnotics].

Zolpidem is a new imidazopyridine hypnotic with a pharmacological profile substantially different from benzodiazepines. In this observational multicenter study the possibility of shifting to zolpidem (10 mg at N1, 15 or 20 after N1) insomniac patients previously taking (for at least 15 days and not longer than 3 months) standard posology of triazolam (0.125-0.25 mg), lorazepam (1 mg) or lormetazepam (1 mg) was assessed. For ethical reasons the patients were mandatorily to be insomniacs despite their taking hypnotics or not tolerating them. Patients enrolled were 299 of whom 276 evaluable (139 males and 136 females; mean age 48.67 +/- 14.64, range 18-83). Study duration was 7 nights with visits at N0 (baseline), N1 (after 1st night), N3 (after 3rd night) and N7 (final evaluation); on each visit the Saint Mary Hospital Sleep Questionnaire and the benzodiazepine withdrawal symptom's rating scale were administered; moreover, after N7, investigators were asked a judgement of feasibility of such a shift. In 229 (83.5%) out of 274 patients such a shift to zolpidem was considered successfully (no occurrence of symptoms and/or signs of previously taken hypnotic withdrawal); in the remaining 45 patients, just 17 (6.2%) seemed to be real unsuccessful cases (reactions mild and transient, anyhow). In conclusion abrupt shift to zolpidem appeared to be largely feasible in the patients studied.

Adolescent↗
PubMed1993

Antifungal agents. VI. In vitro antifungal activities of halobenzoyl esters of cis- and trans-[2-(1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3- dioxolan-4-yl]carbinols.

The synthesis and the in vitro antifungal activities against Candida albicans and Candida spp of a number of halobenzoyl esters of cis- and trans- [2-(1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan -4- yl]carbinols is reported. Some new imidazoles were found more active than ketoconazole and sometimes as potent as bifonazole against Candida albicans. All derivatives were found scarcely active against Candida spp.

Antifungal Agents↗
PubMed1992

Bovine serum amine oxidase: half-site reactivity with phenylhydrazine, semicarbazide, and aromatic hydrazides.

Aromatic hydrazides of the general formula NH2NHCO(CH2)nC6H4R were covalently bound by bovine serum amine oxidase (BSAO), giving rise to optical and CD absorptions at 350-400 nm. Benzohydrazides (n = 0) reacted slowly, in the ratio of one per dimeric protein molecule, like semicarbazide. Phenylacetohydrazides (n = 1) and phenylpropionic hydrazides (n = 2) reacted instead in the ratio of two per dimer, one molecule at a much faster rate than the other. The fast reaction correlated with the loss of enzymatic activity. The contribution to the optical absorbance of either molecule was identical, but only the first one produced a CD band, the wavelength and sign of which were determined by the number n of methylene groups in the hydrazide. In n = 1 and n = 2 compounds, the reaction was faster as the R substituent became more hydrophobic (triazolyl less than imidazolyl less than phenyl), suggesting a specific interaction with the protein matrix. Phenylhydrazine was found to react with the native enzyme in the ratio of only one per protein dimer. However, one phenylhydrazine was also slowly bound by most 1:1 enzyme-hydrazide adducts, with the formation of ternary derivatives. Phenylhydrazine formed the usual intense band at 447 nm with n = 1 and n = 2 hydrazide-BSAO adducts and a weaker, blue-shifted band with the adducts of semicarbazide and of some n = 0 hydrazides. In both cases, the hydrazide absorption band was unaffected. Competition was observed with other benzohydrazides and with the second molecule of n = 1 compounds. A half-site mechanism appears to be operative, the second site being always less reactive than the first. Reactivity and adduct conformation were also affected by N,N-diethyldithiocarbamate, a powerful enzyme inhibitor that binds copper.

Amine Oxidase (Copper-Containing)↗
PubMed1992

Researches on antibacterial and antifungal agents, XIV: Thiophene analogues of bifonazole.

Some thiophene analogues of bifonazole have been synthesized by standard procedures and their antifungal activity has been tested against Candida albicans. Among test derivatives biphenyl-4-yl-5-chloro-thien-2-ylimidazol-1-ylmethane and its 5-deschlorothien-2-yl analogue resulted to be the most active. Their antifungal potency was almost comparable to that of control substances, such as miconazole, ketoconazole, and bifonazole. Replacement of benzene by the pyrrole ring in the biphenyl portion retained almost quantitatively the antifungal activity, whereas substitution with other azoles and with nitrogen alicyclic rings led always to less potent derivatives.

Antifungal Agents↗
PubMed1992

Antibacterial and antifungal agents. XV. Synthesis and antifungal activity of structural analogues of bifonazole and ketoconazole.

The synthesis and antifungal activities of the cis- and trans-1-acetyl-4-[4-[[2-(1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethy l)- 1,3-dioxolan-4-yl]-methoxy]phenyl)piperazines 3 and 4 are reported. Stereochemical assignments to diastereomeric pairs of cis/trans isomers were made on the basis of 1H- and 13C-NMR data. Among test derivatives the best activity was shown by the benzoyl esters of the cis- and trans-[2-(1,1'-biphenyl-4-yl)-2-(1H-imidazol-1-ylmethyl)-1,3-di oxolan-4- yl]methanols 9 and 10.

Antifungal Agents↗
PubMed1992

Safety and diagnostic accuracy of adenosine thallium-201 scintigraphy in patients unable to exercise and those with left bundle branch block.

Three hundred forty consecutive patients (mean age 69 +/- 9 years) were evaluated with adenosine tomographic thallium-201 scintigraphy for suspected coronary artery disease. Minor side effects occurred in 91% of patients. Out of 28 patients (8%) with potentially serious side effects, 28 had significant atrioventricular (AV) block (second-degree, 24 patients; third-degree, four patients; syncope occurred in two patients). Acute bronchospasm and severe refractory angina pectoris occurred in one patient each. All side effects were transient and without sequelae. One hundred twenty-one patients underwent coronary angiography within 9 days of adenosine thallium imaging. The predictive accuracies of adenosine thallium imaging for identifying and localizing ischemia to a specific coronary distribution were: left anterior descending = 88%, left circumflex = 84%, right coronary = 88%. The predictive accuracy of adenosine thallium imaging in patients with left bundle branch block was 91%, and was higher than the 71% predictive accuracy noted in 39 patients who underwent exercise thallium testing (p = 0.04). It is concluded that adenosine thallium-201 myocardial scintigraphy was (1) highly accurate for the detection and localization of significant coronary artery disease; (2) it was more accurate at detecting ischemia in patients with left bundle branch block than exercise thallium testing, and (3) subjective side effects were common and were of no diagnostic importance; transient AV block occurred occasionally.

Adenosine↗
PubMed1991

Narcolepsy and psychopathology. A case report.

The case of a 14-year-old girl presenting with the association of a clearcut narcoleptic syndrome and psychiatric disturbances is reported. Tricyclic anti-depressant drugs and hypnagogic hallucinations seem to play a precipitating role on delusional episodes in a predisposed subject with a positive psychiatric familial history.

Adolescent↗
PubMed1990

Researches on antibacterial and antifungal agents, XII: Analogues of bifonazole with two imidazole moieties and related azoles.

Analogues of bifonazole bearing two imidazole rings and other related azoles have been synthesized and tested as antifungal agents against Candida albicans and Candida spp.. Only a slight part of the antifungal power of the parent drug is retained by some derivatives as evinced by the comparison of new compounds with bifonazole, miconazole, and ketoconazole.

Antifungal Agents↗
PubMed1990

The effect of nocturnal physiological sleep on various movement disorders.

Thirty-one subjects affected by different movement disorders underwent polygraphic and videotape monitoring during nocturnal sleep, to assess movement patterns during the night. It was possible to distinguish two categories of disorders according to their pattern of movements. In the largest group (Meige's syndrome, blepharospasm, amyotrophic choreoacanthocytosis, Tourette syndrome, tonic foot, hemiballism) abnormal movements were still present during sleep, but decreased in frequency and amplitude in all stages. The second group presented three syndromes (nocturnal paroxysmal dystonia, nocturnal myoclonus, restless legs syndrome), in which light non-rapid-eye-movement sleep induced a strong activation of abnormal movements, whereas rapid-eye-movement sleep suppressed them.

Adult↗
PubMed1990

Non-steroidal antiinflammatory agents. VII. Synthesis and antiinflammatory activity of 5-methyl-10,11-dihydro-5H-pyrrolo [1,2-b] [1,2,5]benzotriazepine-11-acetic acid and its 10-aroyl derivatives.

The synthesis of 5-methyl-10,11-dihydro-5H-pyrrolo [1,2-b] [1,2,5]benzotriazepine-11-acetic acid and its 10-aroyl derivatives is reported. Compounds were evaluated for antiinflammatory activity by the carrageenin-induced rat paw edema method. Antinociceptic activity was tested by the hot plate and Randall-Selitto tests. General neuropsychopharmacological effects were also screened. All test compounds showed antiinflammatory effect comparable to that of tolmetin.

Analgesics↗
PubMed1990

Research on psychotropic agents. III. Antidepressant activity and neuropsychobehavioural effects of new 5H-Pyrrolo[1,2-b][1,2,5]benzotriazepine derivatives.

The synthesis of 5H-pyrrolo[1,2-b][1,2,5]benzotriazepine derivatives related to imipramine and aptazepine antidepressant agents is reported. Pharmacological screening on new tricyclic derivatives showed that in some cases antidepressant effects at equimolecular dose with imipramine are associated with sedative-muscle relaxant activities and antinociception.

Animals↗
PubMed1989

Researches on antibacterial and antifungal agents, X. Synthesis and antifungal activities of 1-(p-methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)azoles and some related products.

The synthesis and antifungal activities against Candida albicans and Candida spp. of some pyrrole analogues of bifonazole are reported. 1-(p-Methyl-alpha-[4-(1H-pyrrol-1-yl)phenyl]benzyl)imidazole was found to be equipotent or sometimes superior to bifonazole and ketoconazole, and lightly inferior to miconazole. Substitution of the imidazole moiety with other azoles retained some activities. No activity was shown when the azole aromatic rings were replaced by the heteroalicyclic ones.

Antifungal Agents↗
PubMed1989

Nocturnal complex partial seizures precipitated by REM sleep. A case report.

A 16-year-old patient presenting with complex partial seizures occurring in the transition from a REM period to wakefulness is described. His baseline EEG showed generalized and symmetrical slow spike and wave complexes, on a normal background activity, activated by NREM sleep. Polygraphic and videotape recordings, carried out for several nights, showed that after nearly each REM period, he would wake up briefly, presenting eye blinking followed by a burst of generalized hypersynchronous theta to start his seizures. These were characterized by moaning and autoaggressive behaviour, the ictal EEG showing generalized slow spike and wave complexes in the midst of several movement artifacts. At the end of each fit he fell back to REM sleep. Carbamazepine treatment completely resolved his symptoms, with full normalization of EEG activity.

Adolescent↗
PubMed1989

Paroxysmal electroencephalographic abnormalities genetically transmitted: one family description.

A 10-year-old girl came to our observation since a general rule-out electroencephalogram (EEG) had showed, in absence of any clinical manifestation, generalized and symmetrical 3 c/s spike-and-wave bursts, whose duration was longer than 3 s. The subject, only daughter born from her mother's first marriage, had no family history of neurological diseases; her physical and neuropsychological examinations were normal. A polysomnographic recording showed, during sleep, the same abnormalities observed during wakefulness. Also on this occasion, there were no related clinical manifestations. Subsequent recordings were performed on her 33-year-old mother and on two siblings, 3 and 2 years old, respectively, born from their mother's second marriage, all normal by physical and neuropsychological examinations, with no referral about clinical seizures. Among them, the 3-year-old sister showed asymptomatic left rolandic spikes, while the 2-year-old boy, whose EEG was firstly normal, displayed, 1 year later, a burst of generalized 3 c/s spike-and-wave paroxysmal activity on a 4-7 c/s background activity. The possible unitary genetic transmission of paroxysmal EEG abnormalities is discussed.

Adult↗