Il Farmaco; edizione scientifica最新文献

Dose-related changes of the reduced glutathione were evaluated in forebrains from male Wistar rats aged 10 months after chronic i.p. treatment for two months with the ergot alkaloids dihydroergocristine and dihydroergocriptine. The results indicate that, within a specific dose-range, the concentration of the cerebral reduced glutathione may be modified by exogenous intervention.

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.

We report the results of the antiulcer activity of some arylthiomethylpyridine compounds. Some of these showed gastroprotective activity against 96% ethanol-induced gastric lesions greater than Omeprazole. However they possess antiulcer properties lower than the reference compound against Indomethacin-induced gastric ulcers.

A series of 3-aryl or etheroaryl-6-cyano-7-phenyl-1,2,3,4-tetrahydro-1,2-diazepin- 5-ones was synthesized and evaluated for its antitumor activity against P388 leukemic tumor system in mice. None of the tested compounds showed significant antitumor properties.

A series of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines was synthesised starting from suitable o-benzoylbenzoic acids. The compounds were tested in vitro for inhibition of the specific binding of 3H-Diazepam to benzodiazepine receptors in preparations of membranes from rat brain synaptosomes. None of the compounds was notably active in this test.

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.

The reaction of 3-chloro pyridazines with various amines led to a series of minaprine analogues. Most of them exhibited significant antidepressant activity. The influence of the substituents attached to the pyridazine ring was discussed.

The synthesis of a series of new N,N-disubstituted 4-amino-3-chloroangelicins (4-amino-3-chloro-2H-furo[2,3-h]-1-benzopyran-2-ones) starting from N,N-disubstituted (E)-5-aminomethylene-6,7-dihydrobenzo[b]furan-4(5H)-ones is described. Their capacity of inhibiting DNA synthesis in Ehrlich ascites tumor cells by U.V.-A light irradiation as well as their phototoxic activity on guinea-pig skin have been studied and the data computed by probit analysis; the results are discussed in the light of the modifications introduced in the molecular structure.