Discovery and SAR of benzyl phenyl ethers as inhibitors of bacterial phenylalanyl-tRNA synthetase

A series of benzyl phenyl ethers (BPEs) is described that displays potent inhibition of bacterial phenylalanyl-tRNA synthetase. The synthesis, SAR, and select ADMET data are provided.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-02, Vol.19 (3), p.665-669
Hauptverfasser:	Montgomery, Justin I., Toogood, Peter L., Hutchings, Kim M., Liu, Jia, Narasimhan, Lakshmi, Braden, Timothy, Dermyer, Michael R., Kulynych, Angela D., Smith, Yvonne D., Warmus, Joseph S., Taylor, Clarke
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Triphosphate - chemistry Aminoacyl-tRNA synthetase Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Anti-Infective Agents - chemistry Anti-Infective Agents - pharmacology Antibacterial Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Bacteria Bacteria - enzymology Benzyl phenyl ether Biological and medical sciences Chemistry, Pharmaceutical - methods Drug Design Drug Evaluation, Preclinical - methods FRS Inhibitory Concentration 50 Medical sciences Models, Chemical Pharmacology. Drug treatments Phenyl Ethers - chemistry Phenylalanine-tRNA Ligase - chemistry Phenylalanyl-tRNA synthetase PheRS SAR Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A series of benzyl phenyl ethers (BPEs) is described that displays potent inhibition of bacterial phenylalanyl-tRNA synthetase. The synthesis, SAR, and select ADMET data are provided.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.12.054