Twenty-two 4-aryl/alkyl-1-(diphenylacetyl)thiosemicarbazides were synthesized and their in vitro antibacterial
potency was evaluated. 4-(4-Chlorophenyl)-1-diphenylacetylthiosemicarbazide showed comparable activity to control antibacterial
ampicillin against Gram-positive species with MICs range 3.91-15.63 µg/mL. The compound was also tested
for its cytotoxicity against L929 cell line using the MTT assay technique. The results of antibacterial activity and toxicity
test indicated that it display antibacterial activity at non-cytotoxic concentrations. Finally, some structural and electronic
parameters have been determined in hope to get insight into different biological activity of closely related isomers.
Keywords: Antibacterial activity, Structure-activity relationship (SAR) studies, Thiosemicarbazide derivatives.
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