Structure-based discovery of LpxC inhibitors. Issue 8 (15th April 2017)

• Record Type: Journal Article
• Authors: Zhang, Jing; Chan, Audrey; Lippa, Blaise; Cross, Jason B.; Liu, Christopher; Yin, Ning; Romero, Jan Antoinette C.; Lawrence, Jonathan; Heney, Ryan; Herradura, Prudencio; Goss, Jennifer; Clark, Cynthia; Abel, Cassandra; Zhang, Yanzhi; Poutsiaka, Katherine M.; Epie, Felix; Conrad, Mary; Mahamoon, Azard; Nguyen, Kien; Chavan, Ajit; Clark, Edward; Li, Tong-chuan; Cheng, Robert K.; Wood, Michael; Andersen, Ole A.; Brooks, Mark; Kwong, Jason; Barker, John; Parr, Ian Barrie; Gu, Yugui; Ryan, M. Dominic; Coleman, Scott; Metcalf, Chester A.;
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 8(2017)
• Page Start: 1670
• Page End: 1680
• Publication Date: 2017-04-15
• Subjects: LpxC -- Escherichia coli -- Klebsiella pneumonia -- Pseudomonas aeruginosa -- Acinetobacter baumannii -- Antibacterial; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.03.006
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: The emergence and spread of multidrug-resistant (MDR) Gram negative bacteria presents a serious threat for public health. Novel antimicrobials that could overcome the resistance problems are urgently needed. UDP-3-O-( R -3-hydroxymyristol)- N -acetylglucosamine deacetylase (LpxC) is a cytosolic zinc-based deacetylase that catalyzes the first committed step in the biosynthesis of lipid A, which is essential for the survival of Gram-negative bacteria. Our efforts toward the discovery of novel LpxC inhibitors are presented herein.