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), antimycobacterial (Visual MIC90 5.63 M) and anti-bacterial (restricting S.aureus metabolic activity after 6 h).
Three series of 4-hydroxycoumarin derivatives, comprising a total of 20 novel compounds have been prepared from 2-hydroxyacetophenones. These include a set of 3-[(N-4-benzyloxyphenyl)iminoethyl]-4-hydroxycoumarins, and two differently substituted sets of 3-(1-hydrazonoethyl)-4-hydroxycoumarins. The products were subjected to exploratory biological studies, and some of the compounds exhibited encouraging activity against the trypanosomal parasite T.b. brucei, two of them exhibiting IC50 values of 0.90 μM and 27.88 μM.
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