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Biomedical subjects

F Sparatore

Publications and source records attributed to F Sparatore.

At least 55 records · Page 3Linked to original sources
PubMed1992

Synthesis and evaluation of gastroprotective and antiulcer activity of some 2-substituted-1H-imidazo[4,5-b] pyridines and -1H-benzimidazoles.

Several compounds possessing imidazo[4,5-b]pyridine and benzimidazole structure bearing substituents in position 2 were prepared in order to evaluate an anti-ulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole. Among sixteen compounds taken as representatives of the synthetised series only one (3d) showed a good activity by i.m. administration at 50 mg/kg, while by oral administration of 100 mg/kg a certain number was active and in some cases this activity was quite superior to that of omeprazole.

Animals↗
PubMed1992

Synthesis and choleretic activity of 3-[2-(3-R', 4-R'', 5-R'''-benzyl)-5-R-benzimidazol-1-yl]-butanoic acids.

On the ground of the evidentiated choleretic activity of 3-[2-benzylbenzimidazol-1-yl]butanoic acid, 28 new acids were prepared in order to evaluate the influence of suitable substitutions in either C5 of heteroring or C3', C4', C5' of benzyl group in position 2 on the choleretic activity. Pharmacological results after i.v. administration of 0.5 mmol/Kg in rats confirmed a general high choleretic activity that in eleven cases showed during the first 4 hours an increase of bile volume higher than 80%, that is superior to that produced by dehydrocholic acid. Only in a few cases the bile volume increase was less than 37% of basal value.

Animals↗
PubMed1991

Preparation and pharmacological activity of some 1-lupinylbenzimidazoles and 1-lupinylbenzotriazoles.

Twelve new 1-lupinyl-benzimidazole and 1-lupinyl-benzotriazole derivatives were prepared and, together with some previously described analogues, were tested for analgesic (hot plate test), antiinflammatory (against carrageenan edema), diuretic and antihypertensive (in spontaneously hypertensive rats) activities. Several compounds exhibited a good degree of activity in one or in more than one areas.

Animals↗
PubMed1991

Formamidines with antinociceptive and antiinflammatory activities.

Pursuing our investigations on 7-amino-2,3-polymethyleneindole derivatives, a set of 7-(dimethylaminomethylene)-amino-2,3-polymethyleneindoles, together with some other aryl or cycloalkyl substituted formamidines, were prepared and tested for analgesic and antiinflammatory activities. Several compounds resulted endowed with one or both of these activities; the indole derivatives 1 and 2 exhibited a good degree of both of them.

Amidines↗
PubMed1990

Preparation and antimicrobial activity of 1-arylazo-3,4,6,7,8,9-hexahydroquinolizines.

A set of 1-(R-arylazo)-3,4,6,7,8,9-hexahydroquinolizines, bearing different substituents on the benzene ring, were prepared and tested for antimicrobial activity. These compounds exhibit only a very weak activity against gram-positive and gram-negative bacteria, but are fairly active against several Candida species and other yeast-like fungi.

Anti-Bacterial Agents↗
PubMed1989

Quinolizidine derivatives as potential antitumoral agents.

The activity against lymphocytic leukemia P 388 has been evaluated for thirteen compounds bearing a quinolizidine moiety bound respectively to a phenothiazine nucleus or other isosteric tricyclic systems (12-17), as well to a quinoxalinone (18-20) or an indole (21-24) nucleus. All tested compounds resulted inactive.

Animals↗
PubMed1989

[Preparation and antileukemic activity of quinolizidinylalkyl-derivatives of 4-aminoquinoline and 9-aminoacridine].

By reacting three quinolizidinylalkylamines with 4,7-dichloroquinoline and 6,9-dichloro-2-methoxyacridine six derivatives of 4-aminoquinoline and 9-aminoacridine were obtained. These compounds, which are of interest as potential antibacterial, antiprotozoarian, anti-helminthic and antitumoral agents, so far have been tested against lymphocytic leukemia P 388 and found to be inactive.

Aminoacridines↗
PubMed1989

[Preparation and pharmacologic activity of N-oxides of 4'-(benzotriazol-2-yl-phenylalkanoic and -phenoxyalkanoic acids].

A number of N-oxides of 4'-(benzotriazol-2-yl)-phenylalkanoic and -phenoxyalkanoic acids bearing various substituents on position 6 of benzotriazole together with 4'-(benzotriazol-2-yl) phenylacetic acid were prepared and subjected to a wide pharmacological screening. Several compounds exhibited significant antiinflammatory and diuretic activities, while one was endowed with antihypertensive activity.

Animals↗
PubMed1989

[Preparation and pharmacologic activity of amido- derivatives of 3-methyl-3,4-dihydro benzo- and pyrido-1,2,4-triazin-3-acetic acids].

Thirteen amidoderivatives of 3-methyl-3,4-dihydro-6-R-benzo-1,2,4-triazin-3-yl-acetic acids and of 3-methyl-3,4-dihydro-pyrido [3,2-e]/[3,4-e]-1,2,4-triazin- 3-yl-acetic acids were prepared and submitted to a wide pharmacological screening. The dihydrobenzotriazine and dihydropyridotriazine moieties were endowed with a wide pharmacogenic capacity; in fact, several compounds exhibited high antiinflammatory [(I c), (I d), (II d), (V f), (VI f)], diuretic [(I f), (I g), (I h)] and antihypertensive activities [(I d), (III d)], as well as minor effects on the C.N.S.

Acetates↗
PubMed1988

[Synthesis and pharmacologic activity of 3-quinolizidine-1'-yl-5-R-indoles].

By acid action on the mixture of homolupinal diethylacetal and arylhydrazines several 3-quinolizidin-1'-yl-5-R-indoles (III a - III e) were prepared. The homolupinal diethylacetal, whose hydrolysis gives rise to the unknown aldehyde, was obtained through the action of lupinylmagnesium chloride on diethylphenylorthoformate. Compounds (III) were subjected to wide pharmacological screening; all of them exhibited calcium blocking, negative cardioinotropic and diuretic activities, while single compounds showed antiinflammatory (III d), anticonvulsant and hypoglycemic (III e) activities.

Animals↗
PubMed1988

[Synthesis and pharmacologic activity of 9-R-octahydroindolo[2,3-a]quinolazine].

By acid induced cyclization of quinolizidin-1-one 4-R-phenylhydrazones several derivatives of 1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizine (1), bearing a substituent on position 9, were prepared. When R = Cl this reaction gave rise also to a red-orange compound to which the structure (V) of 1-(p-chloro)phenylazo-3,4,6,7,8,9-hexahydroquinolizine was assigned. Substances (1 b)-(1-f) were tested for spontaneous locomotor, muscle relaxant, analgesic, antiinflammatory, diuretic and cardiovascular activities and for influence on pentylentetrazole and sodium pentobarbital actions. Interesting levels of activity were exhibited in several cases.

Animals↗
PubMed1988

[Analgesic activity of derivatives of 7-amino-2,3-polymethylenindoles and their congeners].

Some N-trifluoromethylsulphonyl and N-trifluoroacetylderivatives of 7-amino-2,3-polymethyleneindoles and of 7-amino-3-propylindole [(I) - (XIII)] were prepared and tested, together with corresponding aniline derivates [(XIV) - (XIX)] and with N-trifluoromethylsulphonylcyclopentylamine (XX), against formic acid induced writhings in mice. With very few exceptions, at the oral dose of 0.167 mmole/kg, they proved from 2 to 3.4 times more active than acetanilide.

Analgesics↗
PubMed1988

[New derivatives of 7-amino-2,3-polymethylenindole with anti-inflammatory activity].

Thirty-four new N-acylderivatives of 7-amino-2,3-polymethyleneinoles (I) and (II) were prepared and tested, together with a few analogues previously obtained, against carrageenan edema in the rat. Several compounds, at a dose of 1 mmole/kg, exhibit good inhibitory activity, that in some cases is superior to that displayed by indomethacin at a dose of 5 mg/kg. With only one exception, activity is confined to compounds of formula (I) and, generally, derivatives of 2,3-hexamethyleneindole are more active than those of lower homologues.

Animals↗
PubMed1988

[Preparation and pharmacologic activity of 2-(4'R')benzyl-5R-benzimidazole. Analgesic activity and effect on conditioned avoidance response].

Several derivatives of 2-benzylbenzimidazole (dibazole) bearing substituents on positions 5 and 4' were prepared and tested, together with dibazole, for their activity on the acquisition of a conditioned avoidance response and for analgesic activity. Chlorpromazine and acetylsalicylic acid were used as standards. Analgesic activity was found for all these compounds, most of which proved more active than A.S.A. As regards the acquisition of a C.A.R., the 5-chloroderivatives exhibit a strong inhibitory activity, that for compound (VIII) is equal to that of chloropromazine, while dibazole and the 5-trifluormethylderivatives stimulate the acquisition.

Analgesics↗