Coumarin and coumarin-3-acetic acid derivatives were synthesized by reacting phenols with malic acid, ethyl acetoacetate and ethyl acetylsuccinate in appropriate reaction conditions.
METHODS AND RESULTS:
All synthesized compounds were subjected to test for their antimicrobial activities against variety of gram positive (Bacillus subtilis, Staphylococcus aureus) and gram negative bacterial stains (Shigella sonnei, Escherichia coli) by agar dilution method. Several of them exhibited appreciable good antibacterial activity against the different strains of gram positive and gram negative bacteria. These findings suggest a great potential of these compounds for screening and use as antibacterial agents for further studies with a battery of bacteria. Minimal inhibitory concentration values shows that experimental compounds were found less active in comparison to standard drug ciprofloxacin but showed parallel activity to moxifloxacin. From table 3, it can be concluded that all the compounds have displayed good activity against B. subtilis.
CONCLUSIONS:
Compounds were enough active against this bacterial strain especially 7-Methoxy coumarin (1), 7-Methyl coumarin (4), 6-methylcoumarin (5), 4,6-Dimethylcoumarin (7), 7-Methoxy-4-methylcoumarin (8) and 7-Methoxy-4-methylcoumarin-3- acetic acid (17). 6-Methylcoumarin (5), 7-methoxy-4- methylcoumarin (8) and 6-aminocoumarin-3-acetic acid (12) showed excellent activities against B. subtilis even better than standard drug amoxifloxacin. |
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