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RESEARCH PRODUCT
ChemInform Abstract: 2-Aryl-Substituted 4H-3,1-Benzoxazin-4-ones as Novel Active Substances for the Cardiovascular System.
U. Rosesubject
BenzoxazinonesStereochemistryArylHalogenationchemistry.chemical_elementIleumGeneral MedicineCalciumPhosphonatechemistry.chemical_compoundmedicine.anatomical_structurechemistryIn vivoCirculatory systemmedicinedescription
4H-3,1-Benzoxazin-4-ones of the structural types 3 and 4 are accessible by cyclization reactions. The introduction of the phosphonate group was achieved by way of Wohl-Ziegler bromination and subsequent Michaelis-Arbuzow reaction with a trialkyl phosphite. Pharmacological investigations on isolated left atria, ileum specimens, and Langendorff hearts as well as in vivo circulatory studies on anesthetized rats revealed that the phosphonates 4 exert calcium antagonistic effects. Whereas 2-(arylvinyl)benzoxazinones gave rise to pronounced negative inotropic effects, compound 3e exhibited relaxing effects on smooth musculature in particular and markedly increased the coronary flow through Langendorff hearts.
year | journal | country | edition | language |
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2010-08-22 | ChemInform |