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Biomedical subjects

A Leonardi

Publications and source records attributed to A Leonardi.

At least 145 records · Page 8Linked to original sources

[Synthesis of benzofuran derivatives with H2 antagonist activity].

N-[2-(7-Dimethylaminomethyl-5-methyl-2-benzofuranmethylthio)ethyl]-N'-methyl-2-nitro-1,1-ethenediamine (III) and N-cyano-N'-[2-(7-dimethylaminomethyl-5-methyl-2-benzofuranmethylthio)ethyl]-N"-methylguanidine (IV) were synthesized. The direct transformation of 2,2-dicarbethoxy-3-hydroxy-5-methyl-7-dimethylaminomethylcoumaran (VII) and of 2,2-dicarbethoxy-3-hydroxycoumaran (XVI) to the corresponding ethyl 2-benzofurancarboxylates (IX) and (XV) is also reported. A mechanism for this reaction is proposed. Compounds (III) and (IV) showed hystamine H2 receptor antagonist activity, but were less potent than cimetidine and ranitidine.

Animals↗

[HLA and Huntington chorea].

Twenty-three patients with documented Huntington's Chorea were typed for 54 HLA antigens belonging to A, B and C loci. The control group was constituted by 124 healthy subjects of the same ethnic background. Patients and controls were typed with the same antisera. In this study no significant differences in the distribution of HLA antigens between the two groups were found. These data indicate that Huntington's Chorea is not associated with any of HLA antigens serologically determined. However, these findings do not exclude the possibility that other genes, whether or not related to MHC, could be responsible of the family inheritance of the disease.

Adult↗

Synthesis and anticonvulsant activity of N-(benzoylalkyl)imidazoles and N-(omega-phenyl-omega-hydroxyalkyl)imidazoles.

A novel series of N-(benzoylalkyl)imidazoles and N-(omega-phenyl-omega-hydroxyalkyl)imidazoles was synthesized and evaluated for anticonvulsant activity in mice against maximal electroshock induced seizures. Some of the compounds showed an activity comparable to or better than phenytoin and phenobarbital. The N-[beta-[4-(beta-phenylethyl)phenyl]-beta-hydroxyethyl]imidazole (38) was selected for further studies; preclinical toxicology and additional efficacy evaluations are in progress. Structure-activity relationships are discussed.

Animals↗

Synthesis and antimycotic activity of alpha-aryl-beta,N-imidazolylalkyl benzyl ethers.

A new series of alpha-aryl-beta,N-imidazolylalkyl benzyl ethers was synthesized and tested for antimycotic and antimicrobial activity. Most of the compounds was highly active in vitro against fungi and gram-positive bacteria. The alpha,4-phenylthiophenyl-beta,N-imidazolylethyl benzyl ether (7) and the alpha,4-biphenyl-beta,N-imidazolylethyl benzyl ether (17) showed higher antifungal activity than 1-[2,4,dichloro-beta-(2,4-dichlorobenzyloxy)phenethyl]imidazole (miconazole) against Candida albicans. None of the compounds was more active than miconazole against Trichophyton mentagrophytes. The most interesting compounds of the series were assayed in vivo, but their activity was inconstant and always lower than that of miconazole.

Animals↗

New alpha-aryl-beta,N-imidzolylethyl benzyl and naphthylmethyl ethers with antimycotic and antibacterial activity.

A new series of alpha-aryl-beta,N-imidazolylethyl benzyl and naphthylmethyl ethers was synthesized and tested for antimycotic and antimicrobial activity. All compounds showed antifungal activity; most of them were also active against gram-positive bacteria, whereas no activity was detected against gram-negative bacteria. Structure-activity relationships are discussed. The alpha-(2,4-dichlorophenyl)-beta,N-imidazolylethyl 4-phenylthiobenzyl ether nitrate (8), which showed good skin tolerability and in vivo antimycotic activity comparable with or better than 1-[2,4-dichloro-beta-(2,4-dichlorobenzyloxy)phenethyl]imidazole (miconazole) and 1-(alpha-(o-chlorophenyl)benzhydryl]imidazole (clotrimazole), was selected for further researches.

Animals↗

[Durene derivates. IV. N-((2,3,5,6-tetramethylbenzoyl)alkyl)imidazoles and N-((beta-(2,3,5,6-tetramethylphenyl)-beta-hydroxy)ethyl)imidazoles with anticonvulsant activity].

A series of N-[(2,3,4,6-tetramethylbenzoyl)alkyl]imidazoles and of N-([beta-(2,3,5,6-tetramethylphenyl)-beta-hydroxy]ethyl)imidazoles has been synthesized. All compounds were tested in mice for anticonvulsant activity against electroshock and pentylenetetrazole convulsions. These durene-derivatives showed good activity, whereas the corresponding benzene-derivatives were inactive.

Animals↗

Thickening of the basement membrane of cortical capillaries in Alzheimer's disease.

Data concerning width and surface of the basement membrane of cortical capillaries in three patients with Alzheimer's disease and five age-matched controls, have been submitted to statistical analysis to ascertain the role of the aging process upon thickening of the basement membrane itself. The analysis showed that there was a significant difference between patients with Alzheimer's disease and controls (P less than 0.01) as to both width and surface of the basement membrane, so suggesting that in these patients aging was not the only factor which thickening of the basement membrane of cortical capillaries was related to.

Age Factors↗

Loss of striatal neurons in Parkinson's disease: a cytometric study.

By means of a cell-counting technique, it has been shown that patients with Parkinson's disease underwent decreased density of striatal nerve cell population. Large cells were more severely affected than small cells. These findings support the view that striatal involvement, although not severe enough to be easily recognized by conventional neuropathological examination, might be responsible of the progressive loss of benefit that most patients experience during chronic L-dopa treatment.

Aged↗

Tendency to periodic recurrence of EEG changes in Lafora's disease. Case report.

A young male patient affected with Lafora's disease and concomitant mental deterioration, myoclonic jerks and epileptic seizures is reported. A cerebral biopsy showed round PAS-positive myoclonus bodies in nerve cells and neuropile. A tendency to periodic recurrence of paroxysmal activity in the EEG tracings, an unusual finding in Lafora's disease, is briefly discussed.

Adolescent↗

Research on durene derivatives. Note I - hypertensive activity of 2-(2,3,5,6-tetramethylbenzyl)imidazoline and related compounds.

A series of substituted 2-(2,3,5,6-tetramethylbenzyl)imidazolines and related compounds have been synthesized to study the steric and hydrophobic effects on the vasoactivity of the introduction of four methyl groups on the phenyl moiety. The 2-(2,3,5,6-tetramethylbenzyl)imidazoline (I) showed a high hypertensive activity, whereas the 2-benzylimidazoline possesses an adrenolytic activity. The 2-(2,3,5,6-tetramethylphenoxy)methylimidazoline (XVII) retained the hypertensive activity, whereas the corresponding thioether (XIX) was inactive. Some structure-activity relationships with regard to the presence of substituents in the 4-position of the phenyl moiety and on the benzylic CH2 are reported.

Animals↗

Early degeneration of the cerebellar cortex, particularly the granular cells.

An 8 month old infant, who died of severe gastroenteritis, presented a degeneration of the cerebellar cortex involving cells arising from the outer granular layer as well as Purkinje and Golgi II cells. Residual Purkinje cells showed vacuolar change of the cell body and dendritic abnormalities. Related lesions were atrophy of the inferior olives and degeneration of the mossy fibers.

Atrophy↗