The synthesis of phenylalanine-derived C5-substituted rhodanines and their activity against selected methicillin-resistant Staphylococcus aureus (MRSA) strains

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• 作者：Diane Hardej ; Charles R. Ashby Jr. ; Nikhil S. Khadtare ; Shridhar S. Kulkarni ; Satyakam Singh ; Tanaji T. Talele
• 关键词：MRSA ; Rhodanine ; Serum
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：December 2010
• 年：2010
• 卷：45
• 期：12
• 页码：5827-5832
• 全文大小：236 K

文摘

A series of rhodanine compounds containing various substituents at the N3- and C5-positions were synthesized and their in vitro activity against a panel of clinically relevant MRSA strains was determined. The anti-MRSA activity of compounds 21 (MIC = 3.9 μg/mL, MBC = 7.8 μg/mL) and 22 (MIC = 1.95 μg/mL, MBC = 7.8 μg/mL) was significantly greater than that of the lead compounds, 1–3 and reference antibiotics penicillin G (MIC = 31.25 μg/mL) and ciprofloxacin (MIC = 7.8 μg/mL) and comparable to that of vancomycin (MIC = 0.97 μg/mL). Compounds 21 and 22 were found to be bactericidal at only 2–4-fold higher than their MIC concentrations. In addition, their MIC values remained unchanged in the presence or absence of 10 % serum. Overall, the results suggest that compounds 21 and 22 may be of potential use in the treatment of MRSA infections.