Synthesis and Biological activities of some Heterocyclics (Paperback)

In the present study, a mild and effective method for the preparation of seven novel pyrazolone derivatives employing phenyl thiosemicarbazide and ethyl acetoacetate as the starting materials is described. The synthesized compounds were characterized by spectral data (1 H-NMR, [13]C-NMR, IR, Mass) and elemental analysis. The compounds were subjected to in-vitro antibacterial activity assays against Escherichia coli, Bacillus anthrecis, Staphylococcus aureus, and Pseudomonas aeruginosa and antifungal activity assays against Candida albicans, Aspergillus niger. The results showed that the synthesized compounds possessed weak to good antibacterial and antifungal activities against the tested bacteria and fungi, with compounds 3a, 3b and 3g displaying good activity. Preliminary bioassays indicated that some of these compounds are also associated with good inhibitory activities against MIC at a concentration of 600µg/mL. Further studies are currently underway to establish a definite structure activity relationship.