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4 results on '"Scarponi U"'

1. Bicyclic compounds with potential antiulcer and/or antisecretory activity. II. 1(or 3),4,6,7-Tetrahydro-1(3)H-pyrano[3,4-d]imidazoles and 1(or 3),4,6,7-tetrahydro-1(3)H-thiopyrano[3,4-d]imidazoles.

Author

Scarponi U, Cimaschi R, Arcari G, Toti D, Ballabio M, Gandini E, and de Castiglione R

Subjects
Animals, Chemical Phenomena, Chemistry, Chemistry, Physical, Gastric Juice metabolism, Guinea Pigs, Imidazoles pharmacology, Mice, Pyrans pharmacology, Rats, Stomach Ulcer etiology, Stomach Ulcer physiopathology, Stress, Psychological complications, Anti-Ulcer Agents chemical synthesis, Imidazoles chemical synthesis, Pyrans chemical synthesis, Stomach Ulcer prevention & control
Abstract

Owing to our current interest in synthesizing and evaluating the antiulcer and antisecretory activity of bicyclic compounds, a series of 1(or 3),4,6,7-tetrahydropyrano- and 1(or 3),4,6,7-tetrahydrothiopyrano-[3,4-d]imidazoles was synthesized and tested. The biological results were compared with those of some previously described 4,5,6,7-tetrahydroimidazo-[4,5-c]pyridine and 4,5,6,7-tetrahydrobenzimidazole derivatives.

Published
1986

3. Byciclic compounds with potential antiulcer and/or antisecretory activity. III--2-substituted tetrahydrothiazolo-[5,4-c]pyridines.

Author

Scarponi U, Lazzarini AM, Caprioli R, de Castiglione R, Toti D, Vaghi F, Castello R, and Ceserani R

Subjects
Animals, Bridged Bicyclo Compounds pharmacology, Chemical Phenomena, Chemistry, Gastric Acid metabolism, Guinea Pigs, Heart drug effects, Heart Rate drug effects, Histamine H2 Antagonists chemical synthesis, In Vitro Techniques, Male, Mice, Muscle, Smooth drug effects, Pyridines pharmacology, Pyridines toxicity, Rats, Rats, Inbred Strains, Thiazoles pharmacology, Thiazoles toxicity, Anti-Ulcer Agents chemical synthesis, Bridged Bicyclo Compounds chemical synthesis, Bridged-Ring Compounds chemical synthesis, Pyridines chemical synthesis, Thiazoles chemical synthesis
Abstract

As the ultimate result of a long-term search for new bicyclic molecules potentially endowed with antiulcer and/or antisecretory activity, simple urea derivatives of 2-guanidino-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine [(VIII), Fig. 1; X = 0, R = alkyl], displaying a strong inhibition of stress- and ASA-induced gastric ulcers and of basal gastric secretion, were found. Their potency does compare very favourably with that of cimetidine and ranitidine and approaches that of famotidine. On spontaneously beating guinea pig atria they behaved as inhibitors of the histamine H2-receptor. In contrast with cimetidine and ranitidine but like other recently described inhibitors (famotidine included), the most active compounds (VIII) caused a surmountable antagonism only at low concentrations and an unsurmountable antagonism at higher concentrations. The onset of action was slow, while the inhibitory effect was hardly reversed by washing. The rational development of the research and the synthetic approach, as well as a quantitative assessment of both in vitro and in vivo potencies in comparison with the best known, clinically used drugs, are shown in detail.

Published
1988

4. Bicyclic compounds with potential antiulcer and/or antisecretory activity. I. 4,5,6,7-Tetrahydrobenzimidazoles.

Author

Scarponi U, Cimaschi R, Rusconi L, Santangelo F, Arcari G, Castello R, Toti D, and de Castiglione R

Subjects
Animals, Anti-Ulcer Agents pharmacology, Anti-Ulcer Agents toxicity, Gastric Juice metabolism, Guinea Pigs, Histamine H2 Antagonists chemical synthesis, Histamine H2 Antagonists pharmacology, Imidazoles pharmacology, Imidazoles toxicity, Lethal Dose 50, Male, Mice, Parasympatholytics chemical synthesis, Parasympatholytics pharmacology, Pyridines pharmacology, Pyridines toxicity, Rats, Rats, Inbred Strains, Structure-Activity Relationship, Anti-Ulcer Agents chemical synthesis, Gastric Juice drug effects, Imidazoles chemical synthesis, Pyridines chemical synthesis
Abstract

The remarkable antiulcer and antisecretory activity of some previously described 4,5,6,7-tetrahydroimidazo[4,5-c]pyridine derivatives prompted us to further investigate related bicyclic systems. Accordingly, a series of 5-amino- and 5-aminomethyl-4,5,6,7-tetrahydrobenzimidazoles, regiospecifically alkylated in position 1, were synthesized and tested. Only a few 1-ethyl-5-amino derivatives displayed a reasonable antiulcer activity in comparison with our former class of compounds.

Published
1985

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