Synthesis, vasodilating and antithrombotic activity of pyridyl-substituted silylisoxazolines
1997; Wiley; Volume: 11; Issue: 10-11 Linguagem: Inglês
10.1002/(sici)1099-0739(199710/11)11
ISSN1099-0739
AutoresE. Lukevics, Māris Vēveris, V. Dirnens,
Tópico(s)Chemical Reactions and Mechanisms
Resumo3-(2-Pyridyl)-5-phenyldimethylsilylisoxazoline, 3-(3-pyridyl)-5-phenyldimethylsilylisoxazoline and 3-(4-pyridyl)-5-phenyldimethylsilylisoxazoline were obtained by the [2+3] cycloaddition reaction of pyridyl nitrile oxides to phenyldimethylvinylsilane. The condensation of 3-pyridyl-substituted 5-triethoxysilylisoxazolines with triethanolamine afforded 3-(2-pyridyl) -5-silatranylisoxazoline, 3-(3-pyridyl)-5-silatranylisoxazoline and 3-(4-pyridyl)-5-silatranylisoxazoline (12). In experiments in vivo and in vitro the vasodilating, antiarrhythmic and antithrombotic properties of pyridyl-substituted silylisoxazolines, their influence on the haemodynamic parameters in anaesthetized animals and their acute toxicity have been studied. It has been found that pyridyl-substituted silylisoxazolines possess vasodilating and antithrombotic properties. In experiments on the noradrenaline-preconstricted isolated rabbit ear artery, 3-(2-pyridyl)- and 3-(4-pyridyl)-5-phenyldimethylsilylisoxazoline exhibited pronounced vasodilating activity. 3-(2-Pyridyl)- and 3-(3-pyridyl)-5-phenyldimethylsilylisoxazoline and 3-(2-pyridyl)-5-silatranylisoxazoline prolonged blood coagulation time. © 1997 John Wiley & Sons, Ltd.
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