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Eur J Med Chem. 2012 May;51:145-53. doi: 10.1016/j.ejmech.2012.02.035. Epub 2012 Feb 25.

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

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1
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA.

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.

PMID:
22405289
PMCID:
PMC3340521
DOI:
10.1016/j.ejmech.2012.02.035
[Indexed for MEDLINE]
Free PMC Article

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