The emergence of pathogens that are resistant to available drug therapies triggered a clear need for the discovery of new antimicrobials rather than analogs of the existing ones. Traditionally, small molecules have been a reliable source for discovering novel biologically active compounds. Among the family of heterocyclic compounds, thiosemicarbazides and their dehydrocyclization products have received attention as possible antimicrobials. Prompted by these findings and in continuation of our efforts in synthesizing new thiosemicarbazide-like compounds with antibacterial activity, novel 1-substituted-4-ethoxycarbonylmethylthiosemicarbazides and their cyclic analogs were synthesized and tested in vitro for their antibacterial potency.

From 18 compounds tested only 3 showed antibacterial activity; 4-ethoxycarbonylmethyl-1-(naphthyl-1ylcarbonyl)-thiosemicarbazide, N-(2-thiohydantoin-3-yl)amide of indole-2-carboxylic acid, and N-(2-thiohydantoin-3-yl)amide of naphthalene-1-carboxylic acid have weak (MICs of 100-400 µg/mL or higher) potency against gram-positive bacteria. All examined compounds were inactive against gram-negative rods.

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