Structure-based discovery of LpxC inhibitors.
Journal: Bioorganic & Medicinal Chemistry Letters
Published:
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.
Authors
Jing Zhang, Audrey Chan, Blaise Lippa, Jason Cross, Christopher Liu, Ning Yin, Jan Antoinette Romero, Jonathan Lawrence, Ryan Heney, Prudencio Herradura, Jennifer Goss, Cynthia Clark, Cassandra Abel, Yanzhi Zhang, Katherine Poutsiaka, Felix Epie, Mary Conrad, Azard Mahamoon, Kien Nguyen, Ajit Chavan, Edward Clark, Tong-chuan Li, Robert Cheng, Michael Wood, Ole Andersen, Mark Brooks, Jason Kwong, John Barker, Ian Parr, Yugui Gu, M Ryan, Scott Coleman, Chester Metcalf