Potent Inhibitors of LpxC for the Treatment of Gram-Negative Infections

In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel series of potent antibacterial LpxC inhibitors represented by hydroxamic acid 1a.

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Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 2012-01, Vol.55 (2), p.914-923
Hauptverfasser:	Brown, Matthew F, Reilly, Usa, Abramite, Joseph A, Arcari, Joel T, Oliver, Robert, Barham, Rose A, Che, Ye, Chen, Jinshan Michael, Collantes, Elizabeth M, Chung, Seung Won, Desbonnet, Charlene, Doty, Jonathan, Doroski, Matthew, Engtrakul, Juntyma J, Harris, Thomas M, Huband, Michael, Knafels, John D, Leach, Karen L, Liu, Shenping, Marfat, Anthony, Marra, Andrea, McElroy, Eric, Melnick, Michael, Menard, Carol A, Montgomery, Justin I, Mullins, Lisa, Noe, Mark. C, O’Donnell, John, Penzien, Joseph, Plummer, Mark S, Price, Loren M, Shanmugasundaram, Veerabahu, Thoma, Christy, Uccello, Daniel P, Warmus, Joseph S, Wishka, Donn G
Format:	Artikel
Sprache:	eng
Schlagworte:	Amidohydrolases - antagonists & inhibitors Animals Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Biphenyl Compounds - chemical synthesis Biphenyl Compounds - chemistry Biphenyl Compounds - pharmacology Catalytic Domain Crystallography, X-Ray Drug Resistance, Bacterial Hydrogen Bonding Hydroxamic Acids - chemical synthesis Hydroxamic Acids - chemistry Hydroxamic Acids - pharmacology Mice Models, Molecular Molecular Conformation Phenyl Ethers - chemical synthesis Phenyl Ethers - chemistry Phenyl Ethers - pharmacology Pseudomonas aeruginosa Pseudomonas Infections - drug therapy Rats Stereoisomerism Structure-Activity Relationship Sulfides - chemical synthesis Sulfides - chemistry Sulfides - pharmacology Sulfones - chemical synthesis Sulfones - chemistry Sulfones - pharmacology
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Beschreibung
Zusammenfassung:	In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel series of potent antibacterial LpxC inhibitors represented by hydroxamic acid 1a.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm2014748