期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 51, 期 -, 页码 145-153出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.02.035
关键词
Thieno[2,3-d]pyrimidinediones; Antibacterial; MRSA; Antibiotic-resistant bacteria; Heterocycle synthesis
资金
- NIAID NIH HHS [R21 AI075239, R21 AI075239-02S1] Funding Source: Medline
- NIGMS NIH HHS [R01 GM087467, R01 GM087467-04] Funding Source: Medline
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. (C) 2012 Elsevier Masson SAS. All rights reserved.
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