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Studies on the Preparation and Biological Activities of 3‐( O ‐Methoxybenzyl)Sydnone Derivatives and 3‐(Fluorophenyl)Sydnones
Author(s) -
Tien HsienJu,
Tsai YanHong,
Yeh WenYuan,
Yeh JongChuan,
Lee YawKuen,
Ho YoungShang
Publication year - 1990
Publication title -
journal of the chinese chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.329
H-Index - 45
eISSN - 2192-6549
pISSN - 0009-4536
DOI - 10.1002/jccs.199000011
Subject(s) - sydnone , chemistry , platelet aggregation , analgesic , biological activity , platelet , organic chemistry , pharmacology , biochemistry , medicine , in vitro , ring (chemistry)
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.