The synthesis and SAR of rhodanines as novel class C β-lactamase inhibitors

β-Lactam antibiotics such as the cephalosporins and penicillins have diminished clinical effectiveness due to the hydrolytic activity of diverse β-lactamases, especially those in molecular classes A and C. A structure–activity relationship (SAR) study of a high-throughput screening lead resulted in...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-10, Vol.10 (19), p.2179-2182
Hauptverfasser:	Grant, Eugene B, Guiadeen, Deodialsingh, Baum, Ellen Z, Foleno, Barbara D, Jin, Haiyong, Montenegro, Deborah A, Nelson, Erin A, Bush, Karen, Hlasta, Dennis J
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents beta-Lactamase Inhibitors beta-Lactamases - classification Biological and medical sciences Drug Evaluation, Preclinical Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Medical sciences Molecular Structure Pharmacology. Drug treatments Piperacillin - antagonists & inhibitors Piperacillin - pharmacology Rhodanine - analogs & derivatives Rhodanine - chemical synthesis Rhodanine - chemistry Rhodanine - pharmacology Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	β-Lactam antibiotics such as the cephalosporins and penicillins have diminished clinical effectiveness due to the hydrolytic activity of diverse β-lactamases, especially those in molecular classes A and C. A structure–activity relationship (SAR) study of a high-throughput screening lead resulted in the discovery of a potent and selective non-β-lactam inhibitor of class C β-lactamases.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(00)00444-3