1. 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