Biomedical subjects

M Satta

Publications and source records attributed to M Satta.

At least 37 records · Page 2Linked to original sources

PubMed1992

Synthesis and pharmacological activity of 4-carbamoyl-5-aryl-6-methyl-4,5-dihydropyridazin-3(2H)-ones.

A new series of 4-carbamoyl-5-aryl-6-methyl-4,5-dihydropyridazin-3(2H)-ones have been synthesized and tested for their antiinflammatory and analgesic properties. Amongst the test compounds, only 31 showed antiinflammatory activity, though of shorter duration than that of indomethacin, taken as reference drug. On the contrary, many derivatives displayed relevant analgesic activity, 4--the only 4,5-dehydroderivative--being the most potent in the writhing test. In the hot plate test 3b, 3f and 3k were found to possess the most significant analgesic properties.

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

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↗

PubMed1991

[Pharmacologic activity of 5-[(dialkylamino)alkyl]-8-chloro-3,5-dihydro-2-methyl/phenyl-4H-pyrido[ 2,3-b][1,4]-diazepine-4-ones].

Some 5-[(dialkylamino)alkyl]-8-chloro-3,5-dihydro-2-methyl/phenyl-4H- pyrido[2,3-b] [1,4]-diazepin-4-ones previously prepared, were subjected to pharmacological experimentation in order to verify variation in biological activity induced by introduction of chlorine on the pyridine nucleus and by replacement of pyridinic with a benzenic ring. The effect upon mice with regard to exploratory activity, motor coordination, spontaneous activity, analgesic activity was tested and their anti-stricnine, anti-cardiazole, anti-amphetamine and anti-reserpine activities were also evaluated. The activities of the texted compounds were compared with those already showed by the analogues unchlorinated derivatives (B) and by isosters benzodiazepinones (D).

Analgesics↗

PubMed1989

[1,4-Disubstituted 1,3-dihydro-2H-1,5-benzo- and chlorobenzodiazepin-2-ones with activity on the central nervous system].

In pursuing the study on pyridodiazepinone derivatives, in order to verify the variation of biological activity induced by replacement of the heteroaromatic with an aromatic nucleus and by the introduction of chlorine on the benzene ring, a series of 1-[(dialkylamino)alkyl]-4-phenyl-1,3-dihydro-2H-1,4-benzodiazepin- 2-ones and of 7-chloro-analogues were prepared. Some benzodiazepinones and their 7-chloro-analagous were subjected to pharmacological experimentation in order to evaluate and compare their effect upon mice with regard to exploratory activity, motor coordination and spontaneous motility. In addition their anti-strychnine, anti-cardiazole, anti-amphetamine and anti-reserpine activities were also evaluated.

Amphetamines↗

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↗

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

[Pyrido[2,3-b][1,4]diazepinones with CNS activity].

In the interests of developing our research on compounds with a pyrazinone nucleus, cyclohomologues, characterised by the presence of one diazepinone nucleus, were prepared. The 5-[(dialkylamino)alkyl]-3,5-dihydro-2-methyl/phenyl-4H-pyrido[2,3- b][1,4]diazepin-4-ones obtained by means of condensation of the 2-(dialkylamino)alkylamino-3-aminopyridines with ethyl acetyl- or benzoyl- acetate, were subjected to pharmacological experimentation in order to evaluate their effect upon mice with regard to exploratory activity, motor coordination, and spontaneous activity. In addition their analgesic activity was evaluated and also their anti-strychnine, anti-cardiazole, anti-amphetamine and anti-reserpine activities.

Amphetamine↗

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↗

PubMed1986

[Effect of mazindol on glucose absorption in everted rat small intestine].

Effect of an anorexiant, mazindol, on glucose absorption was investigated. Ten weeks-old female Sprague-Dawley rats were divided into mazindol treated (fed on powder diet containing 100 mg/kg of mazindol) and control groups. Four weeks later, experiments of continuous observation of glucose absorption and glucose transport were performed in each group using the everted sac method. During 180 min of continuous observation of glucose absorption, significantly lowered glucose concentrations of the serosal medium were observed in the mazindol treated group at oral and caudal ends of the upper, caudal end of the middle, and caudal ends of the lower small intestine, whereas no significant differences in glucose concentrations of the mucosal medium were observed between the two groups. After 60 min incubation for monitoring the glucose transport, significantly decreased glucose concentrations of serosal medium were observed in mazindol treated group at oral and caudal ends of the upper, caudal ends of the middle and caudal ends of the lower small intestine, whereas no significant differences in glucose concentrations of mucosal medium were observed. The results suggested that there is little effect on glucose absorption, but the metabolism of glucose or the remaining glucose in the small intestinal wall is increased by mazindol treatment.

Animals↗

PubMed1986

[Preparation and pharmacologic activity of 1-dimethylaminopropyl-3-methyl-6-chlorquinoxaline-2(1H)-one].

In continuation of previous research 1-dimetilaminopropyl-3-methyl-6-chlorquinoxaline-2(1H)-one was prepared. This compound shows affects on conditioned avoidance response together with analgesic action and inhibition of explorative activity, while it induces only a small degree of motor incoordination and does not protect the animals from toxic doses of strychinine and physostigmine.

Analgesics↗

PubMed1986

[Pharmacologic activity of 1-lupinylquinoxalin-2(1H)-ones, 3,6-disubstituted].

Five 1-lupinyl-3R'-6R"-quinoxalin-2(1H)-ones were tested in mice for acute toxicity, explorative activity inhibition, analgesic activity and for antagonism against physostigmine, strychnine and pentylentetrazol (cardiazol). As reference compounds were used chloropromazine, morphine, atropine and diazepam respectively. All tested compounds inhibit the explorative activity and exhibit high analgesic activity. Compound (I) protects completely the animals from physostigmine toxicity, while compound (IV) antagonizes, although only slightly, all the toxicants tested.

Alkaloids↗

PubMed1986

[Pharmacologic activity of tert-aminoalkyl derivates of quinoxalinone, aza- and diaza-quinoxalinone].

Eight tert-aminoalkyl derivatives of 3-methyl-6R-quinoxalin-2-one, 3-methyl-6/8-azaquinoxalin-2-ones and 3-methyl-6,8-diazaquinoxalin-2-one, previously selected for their deconditioning activity in rats were now tested in mice for analgesic, explorative and incoordinating (muscle relaxant) activities; acute toxicity was also determined. Several compounds show a good degree of activity in the tests used.

Amines↗

PubMed1985

[Anilides with analgesic and antipyretic activity].

Several trimethylcyclopentyl and trimethylcyclopentenyl acetanilides, mono- and di-substituted on the aromatic nucleus as well as the corresponding acyl derivatives from aniline it self and corresponding phenylacetanilides, were prepared and tested as analgesics and antipyretics. Several compounds exhibit considerable activity in some cases superior to that of acetanilide.

Anilides↗

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

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

By condensating ethyl pyruvate with 4-dialkylaminoalkyl-5-aminopyrimidine, obtained by hydrogenolysis of the corresponding 6-chloroderivatives, were prepared 3-methyl-6,8-diazaquinoxalinee-2(1H)-ones which carry on position 1 a tert-aminoalkyl chain (dimethylaminoethyl-, morpholinylethyl-, dimethylaminopropyl- and N-methylpiperazinylpropyl-). The synthetized compounds were tested to verify the effects on acquisition and modification of a conditioned avoidance response (C.A.R.) in rats. In these tests 1-dimethylaminoethyl-3-methyl-6,8-diazaquinoxalin-2(1H)-one, shows activity comparable with that of the cloropromazine.

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↗