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2-Mercaptoacetamidines as gastric antisecretory agents
Journal of Medicinal Chemistry
|March 1, 1979
Summary
New N-substituted 2-mercaptoacetamidines show potent gastric acid inhibition in dogs, acting as a novel class of antisecretory agents. Metabolic conversion and structural modifications impact their effectiveness and potential side effects.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Gastroenterology
Background:
- Gastric acid hypersecretion is a significant medical concern.
- Developing novel agents for gastric acid control is crucial.
Purpose of the Study:
- To synthesize and evaluate N-substituted 2-mercaptoacetamidines for gastric antisecretory activity.
- To identify potent compounds and understand structure-activity relationships.
Main Methods:
- Synthesis of N-substituted 2-mercaptoacetamidines.
- In vivo evaluation of antisecretory activity in gastrin-stimulated dogs.
- Assessment of metabolic interconversion and effects of structural modifications.
Main Results:
- Potent analogues achieved 80-95% inhibition of gastric acid secretion.
- Disulfides showed comparable activity to mercaptoacetamidines, suggesting metabolic conversion.
- Alkylation and higher homologues reduced potency; related compounds had low activity.
Conclusions:
- N-substituted 2-mercaptoacetamidines represent a new structural class with significant gastric antisecretory potential.
- Metabolic interconversion plays a role in activity.
- Observed side effects include emesis, tachycardia, and gastric bleeding.