Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 28, Issue 8, Pages 1298-1302Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.03.023
Keywords
Disulfiram; Disulfides; Antibiotic; Staphylococcus; MRSA; VISA; VRSA
Categories
Funding
- Marshall University School of Pharmacy Faculty Research Support Program
- National Institute of General Medical Sciences [U54GM104942]
- WVU Stroke CoBRE [P20 GM109098]
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [U54GM104942, P20GM109098] Funding Source: NIH RePORTER
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Sixteen disulfides derived from disulfiram (Antabuse (TM)) 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. (C) 2018 Elsevier Ltd. All rights reserved.
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