Studies on WF-5239, a new potent platelet aggregation inhibitor.

Abstract

WF-5239 was produced by a fungal strain identified as Aspergillus fumigatus. The substance was purified by solvent extraction followed by chromatography on silica gel and then crystallized (C9H9NO2, mp [melting point] 142.degree.-145.degree. C). The chemical structure was determined from its physico-chemical properties as N-[2-cis(4-hydroxypheny)ethenyl]formamide. WF-5239 has inhibitory activity against rabbit platelet aggregation induced by arachidonic acid and collagen, with IC50 [median inhibitory concentration] values of 1.25 and 5.0 .mu.g/ml, respectively. Arachidonic acid induced mortality in mice was reduced by a single i.p. dose of WF-5239 (30 mg/kg). These biological properties were compared with those of aspirin.