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The synthesis of new arylpropenones derived from 1-methyl-5-nitro imidazole is described. The investigation of some antiprotozoal properties has shown that compounds with the groups 4-hydroxyphenyl, 4-chlorophenyl or thiophenyl have trichomonacidal activity similar to that of metronidazole.

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.

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.

Neurotensin perfusion into the third ventricle of the unanesthetized rabbit induces an increase of the total power density spectrum of the cortex, without modifying the electrical activity of the cornu Ammonis dorsale. This evidence suggests a direct action of the peptide on the cortical neurons and seems to exclude the involvement of the brainstem reticular formation in inducing the electroencephalographic pattern. Simultaneously Neurotensin produces an evident behavioural excitation and a moderate thermolytic effect. The electroneurophysiologic, autonomic and behavioural changes are independent from one another and seem to depend on an action exerted by Neurotensin at various levels in the CNS.

Esters and amides of N-(3,3-dimethyl-1-triazeno)benzoylamino acids have been synthesized as inhibitors of cell surface neutral proteases. Preliminary data on activity against P-388 lymphocytic leukemia are also reported.

The effect of glucagon on gastric acid secretion was evaluated in conscious cats with gastric fistula and in the isolated gastric fundus from immature rats. Glucagon (10-25 micrograms/kg/h) caused a slight inhibitory effect on pentagastrin-induced acid secretion; in contrast it was ineffective against dimaprit. At these doses glucagon induced a marked increase in glucose plasma levels. In the isolated rat gastric fundus glucagon (10(-7) M-3 x 10(-6) M) induced a concentration-dependent increase in acid output, being approximately 100 times as potent as histamine. Conversely from histamine, glucagon was not affected by pretreatment with phosphodiesterase inhibitors, thus an involvement of cAMP seems to be unlikely.

2,4-Dimethyl-1-oxo-1,2-dihydro-3-carbazoyl-isoquinoline (II), 1-chloro-, 1-methoxy-3-carbazoyl-4-methylisoquinoline (VI, X) and a series of their hydrazonic derivatives have been synthesized and tested in vitro for antibacterial and antifungal activities. 1-(1-Chloro-4-methyl-3-isoquinolinoyl)-2-(5-nitro-2-furfurylide ne) hydrazine (VII h) proved to be the most effective in the series (MIC 0.78 micrograms/ml) and was more potent than furazolidone against several strains of S.aureus; the same compound also showed a moderate antifungal activity.

This paper reports the synthesis of 2- and 4- [benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds and the evaluation of their inhibitory properties against histamine (H1), acetylcholine and barium chloride, on guinea pig isolated ileum. 4-[p.Methoxybenzyl-(2-dimethylaminoethyl)amino]-2-methoxy-pyrimidine (VIII) is shown to possess H1 receptor antagonist activity, with a potency similar to that observed for Tonzylamine. By contrast, a specific, although weak, antimuscarinic effect is displayed by 4-[benzyl-(2-dimethylaminoethyl)amino]-2-methoxy-5-methylthio-pyrimidine (XII).

The synthesis of 1-aryl-5-(1-pyrryl)pyrazoles bearing at position 4 an acetic or alpha-propionic chain is described. The new compounds can be structurally related to lonazolac and its analogues with analgesic-antiinflammatory activities. When tested pharmacologically in comparison with tolmetin and indomethacin none of the above derivatives showed any appreciable activity.

The effect of vasopressin and oxytocin on cerebral electrical activity, somatic behavior, heart rate and rectal temperature of non-anesthetized rabbits was studied. Both peptides induced EEG and behavioral activation and proved to be active in modifying heart rate and rectal temperature. EEG and behavioral changes, as well as autonomic effects seemed to be independent of one another, thus suggesting different points of attack of the peptides at CNS level.