A series of overfifteen newly potential chemotherap eutic agents of hydrazides, hydrazones and imides i ncorporated ibuprofen sub-structure have been synthesized in a very good yield under conventional heat and irradia tion conditions. The microbial inhibitory effect of the new agents has been assessed in vitro against Gram- positive and Gram-negative bacteria as well as antifungal activi ty. Compound 15 showed the highest antibacterial as well as antifungal activities compared to other compounds w ith some antifungal activity higher than standard d rugs. However compound 14 showed the lowest antibacterial activity but simil ar antifungal activity compared to other compounds. All compounds have been characterized by IR, 1 H-NMR, 13 C-NMR and x-ray analyses.