Collect. Czech. Chem. Commun. 1980, 45, 1401-1409

Synthesis of arylacetic acids and their effect on activation of fibrinolysis. Quantitative relations between structure and biological activity

Miroslav Kuchař, Bohumila Brunová, Zdeněk Roubal, Jiří Schlanger and Oldřich Němeček

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3


A series of arylacetic acids, III, has been prepared and evaluated for activation of fibrinolysis and inhibition of heat-denaturation of serum albumin. regression analysis revealed that either activity was influenced mainly by lipophilicity of the aromatic substituents. The graph showing activation of fibrinolysis by acids III takes a linear course up to a maximum, followed by a step decrease. Also included in the series are p-benzyloxy derivatives of the arylacetic acids. Their lipophilicity has been evaluated by thin-layer chromatography, the method of reversed phase being employed. However, the lipophilicity parameters thus obtained fail to describe the hydrophobic bonding of these derivatives to the active site; tabulated values of the parameter π were better in this respect.