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Biomedical subjects

F Sparatore

Publications and source records attributed to F Sparatore.

At least 73 records · Page 4Linked to original sources
PubMed1988

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

Sixteen 2-(4'R')phenyl-5R-benzimidazoles and two 2-(4'-pyridinyl)-5R-benzimidazoles were prepared and tested, together with 2-phenylbenzimidazole, for their activity on the acquisition of a conditioned avoidance response in rats and for analgesic activity in mice, and compared with chlorpromazine and acetylsalicylic acid. Several compounds inhibit strongly the acquisition of a C.A.R., with 2-(4'-alkoxy)phenylbenzimidazoles (XVI) and (XVII) clearly exceeding chlorpromazine. Analgesic activity is also generally present in the examined compounds; those bearing in the position 5 a trifluoromethyl or an acetyl group exhibit an activity higher than that of acetylsalicylic acid. Deconditioning and analgesic activities are not correlated with each other.

Analgesics↗
PubMed1987

[Quinolizidine derivatives with antimicrobial activity].

Thirty quinolizidinyl derivatives, together with two dialkylaminoalkyl analogues, were tested at concentration up to 160 mg/l for antimicrobial activity against 17 microrganisms, including gram-positive and gram-negative strains, Mycobac, tuberculosis, Trichom, vaginalis, fungi and yeasts. The most common activity found is that against Mycobac, tuberculosis, followed by that against gram-positive strains; several compounds [(I a), (I b), (I c), (II a), (III a), (VIII e), (XIX e), (XXI e)] exhibit a good or a very high level of activity. Concerning the gram-negative bacteria, activity is found only against Escherichia coli and is random and usually slight, as is that against fungi, yeasts and protozoa. Compounds (I a), (III a) and (XXI e) are of interest for their high activity and for their broad spectrum of activity, while compound (X e) is peculiar for its selectivity against Mycobac. tuberculosis.

Anti-Bacterial Agents↗
PubMed1987

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

Thirty 3-(2-aryl-5R-benzimidazol-1-yl)butanoic acids were prepared in order to evaluate substitution effects on the 2 and 5 positions of the heterocyclic ring upon the previously recorded choleretic activity of 3-(2-phenylbenzimidazol-1-yl)butanoic acid. A general choleretic activity is shown by the acids tested, which in several cases it is superior to that of the model compound and sometimes also to that of dehydrocholic acid.

Animals↗
PubMed1985

[3,6-disubstituted 1-lupinylquinoxalin-2(1H)-ones of pharmacological interest. Effect on acquisition and modification of a conditioned avoidance response in rats].

Fifteen N-lupinyl derivatives of 3-methyl-, 3-phenyl- and 3-benzylquinoxalin-2(1H)-one, variously substituted on position 6 (R = CH3O, CH3, Cl, CF3), were prepared. Of these, all 1-lupinyl-3-methylquinoxalin-2-ones exhibit a high degree of deconditioning activity in the tests of acquisition and modification of a conditioned avoidance response (C.A.R.) in rats. In both tests, compounds (II) and (IV), with R = CH3O and Cl respectively, proved more active than chloropromazine.

Animals↗
PubMed1983

[Tertiary aminoalkyl derivatives of 3-methyl-6- or -8-azaquinoxalin-2(1H)ones. Effect on acquisition and modification of a conditioned avoidance response in rats].

Eight derivatives of 3-methyl-6-azaquinoxalin-2(1H)-one and of 3-methyl-8-azaquinoxalin-2(1H)-one were prepared. They bear on position 1 an aminoalkyl chain (dimethylaminoethyl, morpholinylethyl, dimethylaminopropyl and N-methylpiperazinylpropyl). Three of these compounds exhibit a high degree of deconditioning activity on rats; compound (I) is particularly active on the acquisition of a conditioned avoidance response, while compound (II) is more active than chloropromazine on the modification of a C.A.R. Compound (II) is characterized also by low toxicity.

Animals↗
PubMed1981

[Alkylation of 6-benzyl-5H-dibenzo(d,f)-(1,3)diazepine].

The alkylation of 6-benzyl-5H-dibenzo(d,f)-(1,3)diazepine (I) with propyl iodide and dimethylaminopropyl chloride in dimethylformamide solution and in the presence of sodium amide was investigated. In both instances the alkylation affected the methylene of benzyl group instead of the cyclic imino group, however the dimethylaminopropyl derivative does not stand the working up conditions, giving place to 2-amino-2'(alpha-phenyl-delta-dimethylamino)valerylamino-biphenyl (III).

Alkylation↗
PubMed1981

[1,6-Disubstituted 3-methylquinoxalin-2(1H)-ones. Effect on acquisition and modification of a conditioned avoidance response in the rat].

Sixteen derivatives of 3-methylquinoxalin-2(1H)-one were prepared; they are variously substituted on position 6 (R = H, COCH3, OCH3, CF3) and bear on position 1 an aminoalkyl chain (dimethylaminoethyl, dimethylaminopropyl, N-methylpiperazinylpropyl and morpholinylethyl). Most of these compounds exhibit a high degree of deconditioning activity on rats; compound (X) is significantly more active than chlorpromazine in the tests used.

Animals↗
PubMed1980

[3,4-Dihydro-1,2,4-benzotriazin-3,3'-spiro steroid derivatives of pharmacological interest].

In order to verify the possibility of pharmacological latentiation of bioactive ketones, the building up of a 3,4-dihydro-1,2,4-benzotriazine ring on position 3, 17 or 20 of steroids with hormonal activity was investigated. The heterocyclic formation was successful only on the less hindered position 3. Four (I alpha, I beta, II alpha, II beta) of the six derivatives so obtained were tested for androgenic activity and their effects were compared with those of testosterone and of the starting ketosteroids (5 alpha- and 5 beta-dihydrotestosterone, 5 alpha- and 5 beta-androstan-3,17-dione). The hormonal activity is not compromised by the coupling of the heterocyclic ring with the steroidal skeleton; on the contrary compound (I beta), derived from the inactive 5 beta-dihydrotestosterone, exhibited a high degree of androgenic activity.

Androstane-3,17-diol↗
PubMed1980

[Derivatives of 2-phenothiazin-2'-yl-cinchoninic acid with analgesic and anti-inflammatory activity].

In order to investigate the effects of the overlapping of cinchophene and phenothiazine structures, connected with antiinflammatory and analgesic activities, several derivatives of 2-phenothiazin-2'-yl-cinchoninic acid were prepared through the condensation of isatin or 5-substituted isatins with 2-acetylphenothiazine or its 10-ter-aminoalkyl derivatives. Most of these compounds exhibit analgesic activity, but only a few, of those so far tested, show antiinflammatory activity. Compound (G) with R' = H, R" = C2H5 and R"' = dimethylaminoethyl shows analgesic activity corresponding to 88% of that of phenylbutazone. Moreover some compounds show signs of sympatholytic and vasodilatatory activities and also bactericidal and amebicidal properties in vitro, while some others demonstrate a modest neuroplegic activity.

Amphetamine↗
PubMed1980

[Preparation of 3,3-disubstituted-3,4-dihydro-1,2,4-benzotriazines].

A compound formerly obtained through the reduction of cyclohexanone o-nitrophenylhydrazone has been defined as cyclohexane-3-spiro-3,4-dihydro-1,2,4-benzotriazine, and its formation has been interpreted via air oxidation of a cyclic form of o-aminophenylhydrazone formed first. The extension of such a reaction to several o-nitrophenylhydrazones of aliphatic, alicyclic and arylaliphatic ketones has been investigated. Formation of 3,4-dihydro-1,2,4-benzotriazines disubstituted in position 3 happens as a general rule; yields are good so long as bulky groups or aromatic nuclei are not close to the hydrazone double bond, hindering the amino group addition either sterically or by charge dispersion. Pharmacological screening has not shown any unusual activity for these new compounds; it is suggested that the formation of dihydrobenzotriazine derivatives be used to latentiate biologically active ketones.

Animals↗
PubMed1979

[Quinolozidinylalkylamines with antihypertensive activity].

Since lupinylamine [(I); R = H] exhibits hypotensive activity, mainly due to ganglionic blocking properties, and it is known that a high degree of steric hindrance around the basic function of other ganglioplegic amines is of paramount importance for optimal activity, several guinolizidine derivatives were prepared. They differ in the length of the alkyl chain connected to the ring and in the position of the amino group along the chain. Some N-substituted derivatives of 2-quinolizidin-1'alpha-yl-ethylamine (II) together with O-lupinylhydroxylamine and 2-quinolizidin-1'beta-yl-ethylamine, respectively isosteric and epimeric to it, were also prepared. When administered orally to spontaneously hypertensive rats, the amines (II), (III) and (XI) produced high and long-lasting antihypertensive activity, while the remaining compounds so far tested were inactive or had only modest effect on blood pressure. Compared with alpha-methyl-DOPA, amine (II) appears to be approximately two to three times as potent. The antihypertensive activity of (II) appears to be linked to glanglionic blocking properties, since this amine proved 1,2 times as potent as mecamylamine in the inhibition of cat nictitating membrane response to stimulation of the preganglionic sympathetic nerve.

Amines↗
PubMed1978

[Benzotriazole derivatives active on plant growth. I. Preparation, characterization, and correlation between physicochemical properties and structure].

Following preliminary observations of auxin-like activity for several benzotriazole derivatives, a large number of new derivatives bearing on position 1 or 2 different kinds of omega-substituted chains were prepared and tested for activity on plant growth. Some physico-chemical properties which are potentially correlated with biological activity were determined for all the new benzotriazole derivatives and for those already studied in this field as growth promoting substances. Partition coefficients (between n-octanol and buffer with pH 5.6) and RM values of 2-substituted isomers were correlated, through regressional analysis, with the corresponding properties of 1-substituted isomers. Finally, the chromatographic characterictics of the sixty substances so far considered were correlated, again through regressional analysis, with the corresponding partition coefficients and with structural features and specific functional groups by which the eventual interactions with the substratum are regulated.

Chemical Phenomena↗
PubMed1978

[Effect of benzotriazole derivatives on plant growth. II].

The action on plant growth of sixty benzotriazole derivatives carrying on position 1 or 2 several kinds of substituents, has been studied via the oat coleoptile section elongation test. At medium and low concentrations almost all compounds behave as activators, while at the highest concentrations many of them, like indolylacetic acid (IAA), are growth inhibitors. It is worth noting the lack of toxicity, even at the highest concentration used, for the 1-hydroxyalkylbenzotriazoles and, more generally speaking, the low toxicity of hydroxyalkylbenzotriazoles and of benzotriazolylalkanoic acid amides. In the range of concentration from 10(-6) to 10(-8) M some methylalkylbenzotriazoles as well as some benzotriazolylalkanoic acids and esters are more active than IAA exhibiting from 40 to 60% of the maximal activity of IAA. The activities of methylalkylbenzotriazoles and particularly that of 2-(1'-methyl)pentylbenzotriazole are outstanding; actually at the lowest concentration tested (10(-8) M and at 10(-5) M, at which concentration this compound shows the maximum activity, the biological responses correspond respectively to more than 50 and 80% of maximal activity of IAA.

Edible Grain↗