Thieno[2,3-d]pyrimidinedione derivatives as antibacterial agents

Mahender B. Dewal, Amit S. Wani, Celine Vidaillac, David Oupický, Michael J. Rybak, Steven M. Firestine

Research output: Contribution to journalArticle

37 Scopus citations

Abstract

Several thieno[2,3-d]pyrimidinediones have been synthesized and examined for antibacterial activity against a range of Gram-positive and Gram-negative pathogens. Two compounds displayed potent activity (2-16 mg/L) against multi-drug resistant Gram-positive organisms, including methicillin resistant, vancomycin-intermediate, vancomycin-resistant Staphylococcus aureus (MRSA, VISA, VRSA) and vancomycin-resistant enterococci (VRE). Only one of these agents possessed moderate activity (16-32 mg/L) against Gram-negative strains. An examination of the cytotoxicity of these agents revealed that they displayed low toxicity (40-50 mg/L) against mammalian cells and very low hemolytic activity (2-7%). Taken together, these studies suggest that thieno[2,3-d]pyrimidinediones are interesting scaffolds for the development of novel Gram-positive antibacterial agents.

Original languageEnglish (US)
Pages (from-to)145-153
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume51
DOIs
StatePublished - May 2012

Keywords

  • Antibacterial
  • Antibiotic-resistant bacteria
  • Heterocycle synthesis
  • MRSA
  • Thieno[2,3-d]pyrimidinediones

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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