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New isosorbide 5-mononitrate derivative with hypotensive activity.
Bollettino Chimico Farmaceutico
|February 1, 1989
Summary
A novel 5-fluoro-nicotinic ester demonstrates significantly enhanced in vitro and in vivo activity compared to isosorbide-5-mononitrate, with improved bioavailability and lower toxicity in rats.
Area of Science:
- Pharmacology
- Medicinal Chemistry
Background:
- Isosorbide-5-mononitrate (5-ISMN) is a widely used vasodilator.
- There is a need for novel vasodilators with improved efficacy and safety profiles.
Purpose of the Study:
- To synthesize and characterize a novel 5-fluoro-nicotinic acid ester derivative.
- To evaluate the pharmacological properties of the new compound, specifically its vasodilatory and hypotensive activities, and compare it to 5-ISMN.
Main Methods:
- Synthesis of the 5-fluoro-nicotinic ester with isosorbide-5-mononitrate.
- In vitro assessment of vasodilatory activity using rabbit aortic helical strips.
- In vivo evaluation of hypotensive activity in guinea-pigs.
- Pharmacokinetic and toxicological studies in rats after oral administration.
Main Results:
- The novel ester (compound 3) exhibited five times higher in vitro activity than 5-ISMN.
- Compound 3 demonstrated markedly superior hypotensive activity in guinea-pigs compared to 5-ISMN.
- In rats, compound 3 showed inferior bioavailability but lower acute toxicity than 5-ISMN after oral administration.
Conclusions:
- The synthesized 5-fluoro-nicotinic ester represents a promising novel vasodilator candidate.
- The compound offers enhanced potency and potentially improved safety profile over existing treatments.
- Further investigation is warranted to explore its therapeutic potential.