Showing papers by "Giuseppe Paglietti published in 1994"

Choleretic activity of 3-[ring substituted benzotriazol-1(2)-yl]alkanoic and alkenoic acids.

Abstract: In order to investigate the influence of structural modifications on the high choleretic activity of 3-(benzotriazol-1-yl)butanoic acid, a set of new benzotriazolyl alkanoic and alkenoic acids was prepared and, together with some other acids previously described, tested in rats by i.v. administration at the dose of 0.5 mmol/kg. Most of the tested compounds exhibited a good choleretic activity comparable with or higher than that of the model acid and of dehydrocholic acid (+56% mean increase of bile volume during 4 hours). Influence of nature and position of substituents was shown in some cases: a moderate decrease of activity was observed for methoxy derivatives and for the introduction of a methyl group in position 6, while a trifluoromethyl group in the same position enhanced the activity (10). Activity was maintained after the introduction of unsaturation in the chain (17,18), but was completely suppressed when unsaturation was associated with a shortening of the alkenoic chain (16). Moving the butanoic chain from position 1 to position 2 in the case of the nitroderivative (15) produced a striking increase of activity (from +42 to +118 mean variation of bile volume during 4 hours), while the same change in the unsubstituted acid 1 abolished the activity.

Synthesis of 1-Methyl-2,3-dimethyl-N(isopropyl)carbamates-4,5-dihydro- 7-R′-8-R-1H-benzo(g)indoles and Evaluation of in vitro Anticancer Activity.

Abstract: The synthesis of 7-mono or 7,8-disubstituted 4,5-dihydro-1-methyl-1H- benzo[g]indoles bearing a methyl-N-isopropylcarbamate group in position 2 or 2,3 of the pyrrole ring is described, in order to evaluate in vitro, anticancer activity. The preliminary results of this screening at the NCI of Bethesda showed a certain cellular subpanel selectivity between 10(-5) and 10(-4) molar concentrations.

Synthesis of 1-methyl-2,3-dimethyl-N(isopropyl)carbamates-4,5-dihydro-7-R'- 8-R-1H-benzo[g]indoles and evaluation of in vitro anticancer activity.

Abstract: The synthesis of 7-mono or 7,8-disubstituted 4,5-dihydro-1-methyl-1H- benzo[g]indoles bearing a methyl-N-isopropylcarbamate group in position 2 or 2,3 of the pyrrole ring is described, in order to evaluate in vitro, anticancer activity. The preliminary results of this screening at the NCI of Bethesda showed a certain cellular subpanel selectivity between 10(-5) and 10(-4) molar concentrations.

Synthesis and Evaluation of Gastroprotective Activity of Omeprazole Related Benzimidazole, Imidazo(4,5-b)pyridine and Quinoxaline 2- Substituted Derivatives.

Abstract: Twenty compounds possessing benzimidazole, imidazo[4,5-b]pyridine and quinoxaline structure bearing either a substituted arylmethylmercapto- or an arylmethylsulfinyl group in position 2 were prepared in order to evaluate an antiulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole at the dose of 50 mg/kg after i.m. administration. One third of these compounds showed a moderate activity, being about half potent as omeprazole.

Synthesis and Evaluation of Gastroprotective and Antiulcer Activity of Some 2-Substituted 1H-Imidazo(4,5-b)pyridines and -1H-benzimidazoles.

Abstract: Several compounds possessing imidazo[4,5-b]pyridine and benzimidazole structure bearing substituents in position 2 were prepared in order to evaluate an anti-ulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole. Among sixteen compounds taken as representatives of the synthetised series only one (3d) showed a good activity by i.m. administration at 50 mg/kg, while by oral administration of 100 mg/kg a certain number was active and in some cases this activity was quite superior to that of omeprazole.