Benzylidene Rhodanines as Novel Inhibitors of UDP- N-Acetylmuramate/ l-Alanine Ligase

Benzylidene rhodanines are novel inhibitors of UDP N-acetylmuramate/ l-alanine ligase. They showed selective whole-cell activity against the Gram-positive MRSA but not against the Gram-negative Escherichia coli. Their cytotoxic effect on mammalian CHO cells was also evaluated. Benzylidene rhodanine...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2002-02, Vol.12 (4), p.697-699
Hauptverfasser:	Sim, Mui Mui, Ng, Siew Bee, Buss, Antony David, Crasta, Sharon Carmelita, Goh, Kah Lin, Lee, Sue Kim
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Benzylidene Compounds - chemical synthesis Benzylidene Compounds - pharmacology Biological and medical sciences Cell Survival - drug effects CHO Cells - drug effects Cricetinae Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Gram-Negative Bacteria - drug effects Gram-Positive Bacteria - drug effects Medical sciences Microbial Sensitivity Tests Peptide Synthases - antagonists & inhibitors Pharmacology. Drug treatments Rhodanine - chemical synthesis Rhodanine - pharmacology
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Zusammenfassung:	Benzylidene rhodanines are novel inhibitors of UDP N-acetylmuramate/ l-alanine ligase. They showed selective whole-cell activity against the Gram-positive MRSA but not against the Gram-negative Escherichia coli. Their cytotoxic effect on mammalian CHO cells was also evaluated. Benzylidene rhodanine 1 inhibits MurC (IC 50=27 μM) and shows whole-cell activity against MRSA (MIC=31 μM).
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00832-0