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The synthesis of phenylalanine-derived C5-substituted rhodanines and their activity against selected methicillin-resistant Staphylococcus aureus (MRSA) strains by Diane Hardej; Charles R. Ashby Jr.; Nikhil S. Khadtare; Shridhar S. Kulkarni; Satyakam Singh; Tanaji T. Talele is a Chemistry article available to read on EtoBox.

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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 1⁄4 3.9 mg/mL, MBC 1⁄4 7.8 mg/mL) and 22 (MIC 1⁄4 1.95 mg/mL, MBC 1⁄4 7.8 mg/mL) was significantly greater than that of the lead compounds, 1e3 and reference antibiotics penicillin G (MIC 1⁄4 31.25 mg/mL) and ciprofloxacin (MIC 1⁄4 7.8 mg/mL) and comparable to that of vancomycin (MIC 1⁄4 0.97 mg/mL). Compounds 21 and 22 were found to be bactericidal at only 2e4-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.

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Author

Diane Hardej; Charles R. Ashby Jr.; Nikhil S. Khadtare; Shridhar S. Kulkarni; Satyakam Singh; Tanaji T. Talele

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)

Published

2010

Language

EN

Field

Chemistry (Physical Sciences)