Studies on the Preparation and Biological Activities of 3‐( O ‐Methoxybenzyl)Sydnone Derivatives and 3‐(Fluorophenyl)Sydnones

Two new sydnones; 3‐( o ‐methoxybenzyl)sydnone(1) and 3‐( o ‐melhoxybenzyl)‐4‐morpholinomethylsydnone(2) were synthesized from o ‐methoxybenzylamine and ethyl bromoacetat in moderate yields. 3‐( o‐,m‐,p ‐Fluorophenyl)sydnones were prepared from the corresponding fluoroaniline and chloroacetic acid in higher yields with a conventional method. From the biological activity test, 1 shows significant response of coronary dilation test, collagen induced platelet aggregation inhibition, local anesthetic and moderate cardiotropic activity. In addition, 1 also leads to anticonvuls, muscle relaxation and behavior depression. But 2 only shows inhibition of collagen induced platelet aggregation and antiwrithing. 3‐( p ‐Fluorophenyl)sydnone (5) shows significant response of coronary dilation, collagen induced platelet aggregation inhibition, moderate cardiotropic activity, antiwrithing and local anesthetic But 3‐( o ‐Fluorophenyl)sydnone(3) and 3‐( m ‐fluorophenyl)sydnone(4) only show coronary dilation and moderate cardiotropic activity.