Search PubMed⌕ Search

Biomedical subjects

E Marmo

Publications and source records attributed to E Marmo.

At least 55 records · Page 3Linked to original sources
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↗
PubMed1989

Research on heterocyclic compounds. XXV. Phenyl derivatives of fused imidazole systems: antiinflammatory activity.

A group of seven acidic phenyl derivatives of some fused imidazole systems were subjected to a series of tests in vivo in order to evaluate their pharmacological activity. Antiinflammatory activity was studied by means of the carrageenin-induced rat paw edema. Hot plate test and writhing induced by acetic acid in mice were used to evaluate analgesic activity. Yeast-induced hyperthermia in rats was employed to study antipyretic action. Irritative and ulcerogenic action on the rat gastric mucosa was examined at higher doses. The antiaggregating activity and the inhibition of platelet malondialdehyde production were studied in vitro. All experimental results are discussed from the point of view of structure-activity relationships and mode of action.

Animals↗
PubMed1989

Amides of 1,3,3-trimethyl-n-[(2-pyridyl)methyl]-2-oxabicyclo [2.2.2]octan-6-amine with depressant and antiarrhythmic activities.

The synthesis of 1,3,3-trimethyl-N-[(2-pyridyl)methyl]-2- oxabicyclo [2.2.2]octan-6-amine (II) (exo, endo mixture) starting from 1,3,3-trimethyl-N-nitro-2-oxabicyclo [2.2.2]octan-6-imine (I), as well as of a series of amides (III) derived from the above amine, is described. Some compounds (III) showed remarkable depressant and antiarrhythmic activities in rats and mice, respectively, whereas the clofibric acid amide (III e) showed an appreciable hypolipidemic activity in rats. Moreover, the above compounds usually exhibited a moderate infiltration anesthesia in mice, as well as a weak hypotensive and bradycardic activity in rats.

Amides↗
PubMed1988

Prenatal and postnatal thallium exposure in rats: effect on development of vasomotor reactivity in pups.

Vasomotor reactivity has been evaluated in rats exposed perinatally and postnatally to thallium sulphate (1 mg/dl in their drinking water ad libitum). Prenatal and postnatal exposure to thallium did not modify the values of the systolic arterial blood pressure on the 30th and 60th day in pups of normotensive and DOCA-hypertensive rats. The hypertensive responses induced by endosinusal carotid hypotension and by 1-noradrenaline in pups of normotensive and DOCA-hypertensive rats, exposed or not exposed to thallium sulphate, were more intensive on the 60th than on the 30th day. Similar effects were observed for the hypotensive responses induced by 1-isoprenaline and acetylcholine. Prenatal exposure to thallium did not modify hypertensive responses induced by endosinusal carotid hypotension on the 30th and 60th days, but it caused a decrease of hypertensive responses induced by 1-noradrenaline on the 30th and 60th days and hypotensive responses induced by 1-isoprenaline and acetylcholine exclusively on the 60th day. Postnatal exposure to thallium did not modify hypertensive responses induced by endosinusal carotid hypotension and hypotensive responses induced by acetylcholine, but it caused a decrease of hypertensive responses induced by 1-noradrenaline on the 30th and 60th days in pups of normotensive rats and exclusively on the 60th day in pups of DOCA-hypertensive rats. Moreover, postnatal exposure to thallium caused a decrease of the hypotensive response induced by 1-isoprenaline exclusively on the 60th day. Our findings show that prenatal and postnatal exposure to thallium sulphate modifies the rat's developing vascular autonomic nervous system with a reduction of the alpha, beta-adrenergic and muscarinic vasomotor reactivity.

Animals↗
PubMed1988

Glutamergic transmission and cardiovascular apparatus in normotensive rats.

The cardiovascular effects induced by L-glutamic acid (G) on the cardiovascular apparatus of normotensive ethyl urethane-anaesthetized rats have been evaluated. (a) When administered i.v. (1 to 100 mg/kg) G induced a transitory and dose-dependent increase of arterial pressure (AP) with very moderate sinus bradycardia. It was antagonized by L-glutamic acid diethyl ester (GDEE, 0.1 to 100 mg/kg i.v.). (b) The intracerebroventricular (i.c.v.) administration of G (third ventricle, right lateral ventricle, posterior hypothalamus and striatum) at a dose of 0.1 to 10 mg/an induced a transitory and dose-dependent increase of AP, abolished by i.c.v. GDEE (1 to 10 mcg/an). (c) G hypertension was reduced by several procedures, i.e. catecholamine depletion, alpha 1, alpha 1 and alpha 2 or beta adrenergic blocks, alpha 2 central adrenergic stimulation, Ca2+ transmembrane or gangliary block, surrenectomy, and spinal transection at C7. (d) Atropine, bilateral vagotomy and sinus carotidal denervation increased G hypertension. (e) Therefore the bradycardia does seem to be due to a reflex-mediated effect via sinus carotid and aortic baroreceptors. (f) These data show that glutamergic transmission also participates through a central mechanism in the regulation of cardiovascular function in rats, via an increase in central sympathetic efferent activity.

Animals↗
PubMed1988

Research on heterocyclic compounds. XXIV. Antiinflammatory activity of some imidazo[1,2-c]pyrimidine derivatives.

A group of four acidic imidazo[1,2-c]pyrimidine derivatives were subjected to a series of tests in vivo in order to assess their pharmacological activity. Antiinflammatory activity was studied by means of the carrageenin-induced paw edema and pleurisy in rats. Hot plate test and writhing induced by acetic acid in mice were employed to evaluate analgesic activity, whereas the yeast-induced hyperthermia in rats was used to study antipyretic activity. The irritative and ulcerogenic action on the rat gastric mucosa was examined at higher doses. The inhibitory activity on the platelet malondialdehyde production was studied in order to obtain information about the mechanism of action of test compounds.

Acetates↗
PubMed1988

3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities.

The synthesis of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole (II) and its 4-bromo derivative (III) starting from chalcone epoxide, as well as of a series of esters and N-substituted carbamates derived from (II) and (III), is described. Some of these compounds showed remarkable depressant, antiarrhythmic and analgesic activities in mice and rats. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardic and antiinflammatory activities in rats, infiltration anesthesia and hypoglycemic activity in mice, as well as a weak platelet antiaggregating activity in vitro.

Analgesics↗
PubMed1988

3,5-Diphenyl-1H-pyrazole derivatives. II--N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives with analgesic and other activities.

The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.

Analgesics↗
PubMed1988

N,N-disubstituted 4-amino-(6-methoxy)-3-phenyl-2H-naphtho [1,2-b]pyran-2-ones with antiarrhythmic, platelet antiaggregating and local anesthetic activities.

The synthesis of title compounds (VI) by 1,4-cycloaddition of phenylchloroketene to N,N-disubstituted (E)-2-aminomethylene-3,4-dihydro-(6-methoxy)-1(2H)naphthalenones, followed by dehydrochlorination with DBN and dehydrogenation with Pd/C of the resulting cycloadducts, is described. Some compounds (VI) showed antiarrhythmic activity in rats higher or like that of quinidine and platelet antiaggregating activity in vitro like that of acetylsalycilic acid, as well as moderate infiltration anesthesia in mice and weak hypotensive, bradicardic and antiinflammatory activities in rats.

Anesthetics, Local↗
PubMed1988

Aminoethers of 1,3,3-trimethyl-5-(phenylmethylene)-2-oxabicyclo[2.2.2]octan-6-h ydroxy imine with antiarrhythmic activity.

The synthesis of beta-dialkylaminoethyl ethers (III a-f) and gamma-dialkylaminopropyl ethers (III g-l) starting from 1,3,3-trimethyl-5-(phenylmethylene)-2-oxabicyclo[2.2.2]octan-6- hydroxyimine (II) is described. beta-Diisopropylaminoethyl ether (III b) and gamma-piperidinopropyl ether (III i) showed an antiarrhythmic activity in rats similar to that of quinidine. Moreover, a number of ethers (III) showed weak hypotensive and bradycardic activity in rats and moderate infiltration anesthesia in mice.

Anesthetics, Local↗
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

Ureas and amides derived from N-(5-norbornen-2-ylmethyl) bornan-2-exo-amine with antiarrhythmic and other activities.

The synthesis of title compounds by reaction of camphor nitrimine with (5-norbornen-2-yl)methylamine, followed by NaBH4 reduction of the resulting imine to N-substituted isobornylamine (IV) and reaction of (IV) with alkyl and aryl isocyanates or acyl chlorides, is described. Some ureas and amides are endowed with antiarrhythmic activity in rats superior or comparable to that of quinidine, whereas benzamide (V o) showed an appreciable hypoglycemic activity in mice. Moreover, compounds (V) exhibited in general moderate hypotensive, bradycardic and antiinflammatory activities in rats, as well as a weak infiltration anesthesia in mice.

Amides↗
PubMed1987

1-substituted 5-dialkylaminomethyl-1,5,6,7-tetrahydroindazol-4-ones with antiinflammatory and analgesic activity.

The synthesis of 1-phenyl- and 1-methyl-5-dialkylamino-methyl-1,5,6,7-tetrahydroindazol-4-ones (III) and (IV) by Mannich reaction of the corresponding 1-substituted 1,5,6,7-tetrahydroindazol-4-ones (I) and (II) is described. Some compounds (III) showed a good antiinflammatory and analgesic activity in rats and mice, respectively. Infiltration anesthesia in mice and antiacetylcholine activity in vitro are also reported.

Acetylcholine↗