Premium
Synthesis, vasodilating and antithrombotic activity of pyridyl‐substituted silylisoxazolines
Author(s) -
Lukevics E.,
Veveris M.,
Dirnens V.
Publication year - 1997
Publication title -
applied organometallic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.53
H-Index - 71
eISSN - 1099-0739
pISSN - 0268-2605
DOI - 10.1002/(sici)1099-0739(199710/11)11:10/11<805::aid-aoc637>3.0.co;2-e
Subject(s) - antithrombotic , chemistry , vasodilation , in vivo , pharmacology , nitrile , stereochemistry , medicine , organic chemistry , microbiology and biotechnology , biology
3‐(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.