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ID: ALA4219167

Journal: Bioorg Med Chem Lett

Title: Disulfiram-based disulfides as narrow-spectrum antibacterial agents.

Authors: Sheppard JG, Frazier KR, Saralkar P, Hossain MF, Geldenhuys WJ, Long TE.

Abstract: Sixteen disulfides derived from disulfiram (Antabuse™) were evaluated as antibacterial agents. Derivatives with hydrocarbon chains of seven and eight carbons in length exhibited antibacterial activity against Gram-positive Staphylococcus, Streptococcus, Enterococcus, Bacillus, and Listeria spp. A comparison of the cytotoxicity and microsomal stability with disulfiram further revealed that the eight carbon chain analog was of lower toxicity to human hepatocytes and has a longer metabolic half-life. In the final analysis, this investigation concluded that the S-octylthio derivative is a more effective growth inhibitor of Gram-positive bacteria than disulfiram and exhibits more favorable cytotoxic and metabolic parameters over disulfiram.

CiteXplore: 29571571

DOI: 10.1016/j.bmcl.2018.03.023