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

被引：80

作者：

Brown, Matthew F. ^{[1
]}

Reilly, Usa ^{[1
]}

Abramite, Joseph A. ^{[1
]}

Arcari, Joel T. ^{[1
]}

Oliver, Robert ^{[1
]}

Barham, Rose A. ^{[1
]}

Che, Ye ^{[2
]}

Chen, Jinshan Michael ^{[1
]}

Collantes, Elizabeth M. ^{[2
]}

Chung, Seung Won ^{[1
]}

Desbonnet, Charlene ^{[3
]}

Doty, Jonathan ^{[1
]}

Doroski, Matthew ^{[1
]}

Engtrakul, Juntyma J. ^{[4
]}

Harris, Thomas M. ^{[1
]}

Huband, Michael ^{[3
]}

Knafels, John D. ^{[5
]}

Leach, Karen L. ^{[4
]}

Liu, Shenping ^{[5
]}

Marfat, Anthony ^{[1
]}

Marra, Andrea ^{[3
]}

McElroy, Eric ^{[1
]}

Melnick, Michael ^{[1
]}

Menard, Carol A. ^{[6
]}

Montgomery, Justin I. ^{[1
]}

Mullins, Lisa ^{[3
]}

Noe, Mark. C. ^{[1
]}

O'Donnell, John ^{[3
]}

Penzien, Joseph ^{[3
]}

Plummer, Mark S. ^{[1
]}

Price, Loren M. ^{[1
]}

Shanmugasundaram, Veerabahu ^{[2
]}

Thoma, Christy ^{[3
]}

Uccello, Daniel P. ^{[1
]}

Warmus, Joseph S. ^{[1
]}

Wishka, Donn G. ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Worldwide Med Chem, Groton, CT 06340 USA

[2] Pfizer Global Res & Dev, Computat Chem, Groton, CT 06340 USA

[3] Pfizer Global Res & Dev, Antibacterials Res Unit, Groton, CT 06340 USA

[4] Pfizer Global Res & Dev, Drug Metab, Groton, CT 06340 USA

[5] Pfizer Global Res & Dev, Struct Biol, Groton, CT 06340 USA

[6] Pfizer Global Res & Dev, Primary Pharmacol, Groton, CT 06340 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷 / 02期

关键词：

ZINC-DEPENDENT DEACETYLASE; PLASMA-PROTEIN BINDING; UDP-3-O-(R-3-HYDROXYMYRISTOYL)-N-ACETYLGLUCOSAMINE DEACETYLASE; PSEUDOMONAS-AERUGINOSA; CRYSTAL-STRUCTURE; BAD BUGS; BIOSYNTHESIS; ANTIBIOTICS; MECHANISM; DESIGN;

D O I：

10.1021/jm2014748

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：914 / 923

页数：10

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