Convergent synthesis and biological evaluation of 3[2-(benzylidenehydrazinyl]thiazol-4-yl]-4-hydroxycoumarins

A convenient synthesis of a small library of 4-hydroxycoumarin derivatives, containing thiazole and benzylidenehydrazine moieties has been achieved, using 2-hydroxyacetophenone and aryl- and heteroaryl aldehydes as starting materials. In vitro biological studies revealed that some of the compounds exhibited modest activities, viz.; anti-malarial (65% PLDH viability), anti-trypanosomal (52% T.b.brucei viability), anti-mycobacterial (Visual MIC90 5.63 mu M) and anti-bacterial (restricting S.aureus metabolic activity after 6 h). [GRAPHICS] .