Abstract
Several bicyclic dihydropyrimidines were synthesized and evaluated for their calcium antagonistic activities by comparison with the usual 1,4-dihydropyridine calcium antagonist reference compound nifedipine. The solid-state structure of the isopropyl 2-methyl-4-(3'-nitrophenyl)-1,4-dihydrobenzo[4,5]imidazo[1,2- a]pyrimido-3-carboxylate shows that these compounds can adopt the most important structural features of the 1,4-dihydropyridine and 1,4-dihydropyrimidine calcium channel blockers. The high-potassium depolarized rat aorta assay was used for testing the compounds as calcium channel blockers. Some compounds showed interesting vasorelaxant activity.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Aorta, Thoracic / drug effects
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Calcium Channel Blockers / chemical synthesis
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Calcium Channel Blockers / chemistry
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Calcium Channel Blockers / pharmacology*
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Crystallography, X-Ray
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Drug Evaluation, Preclinical
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In Vitro Techniques
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Magnetic Resonance Spectroscopy
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Male
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Models, Molecular
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Molecular Structure
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Vasodilator Agents / chemical synthesis
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Vasodilator Agents / chemistry
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Vasodilator Agents / pharmacology
Substances
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Calcium Channel Blockers
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Pyrimidines
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Vasodilator Agents