Thiosemicarbazide derivatives are important class of biologically active compounds that exhibit an impressive array of promising biological properties including antiviral, anticonvulsant, antituberculosis, analgesic, antibacterial, antifungal, and anticancer activities. Among them, their antimicrobial properties have been extensively described and systematically studied in our research group.

Twenty-two 1-diphenylacethyl-4-aryl/alkyl-thiosemicarbazides were synthesized and their in vitro antibacterial potency was evaluated. Among studied compounds, 4-(4-chlorophenyl)-1-diphenylacethyl thiosemicarbazide showed activity comparable to control antibacterial ampicillin at non-toxic concentration. Thus, it potency and low toxicity makes it valid lead for synthesizing new compounds with better bioactivity.

Fianlly, some structural and electronic parameters have been determined in hope to get insight into different biological activity of close related isomers. Based on computational studies some SAR trends can be summarized as follows: (i) electron-withdrawing substitution seems to be better than electron-donating, (ii) para-position tends to be better than ortho or meta, (iii) antibacterial response is correlated rather with electronic than structural parameters.

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