@article{c33c1fc8e72f4b7b90a911642aee06a2,
title = "Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design",
abstract = "The ATPase subunit of DNA gyrase B is an attractive antibacterial target due to high conservation across bacteria and the essential role it plays in DNA replication. A novel class of pyrazolopyridone inhibitors was discovered by optimizing a fragment screening hit scaffold using structure guided design. These inhibitors show potent Gram-positive antibacterial activity and low resistance incidence against clinically important pathogens.",
keywords = "Antibacterials, DNA gyrase B, fragment-based drug design, structure-based drug design",
author = "Cross, {Jason B.} and Jing Zhang and Qingyi Yang and Mesleh, {Michael F.} and Romero, {Jan Antoinette C.} and Bin Wang and Doug Bevan and Poutsiaka, {Katherine M.} and Felix Epie and Terence Moy and Anu Daniel and Joseph Shotwell and Brian Chamberlain and Nicole Carter and Ole Andersen and John Barker and Ryan, {M. Dominic} and Metcalf, {Chester A.} and Jared Silverman and Kien Nguyen and Blaise Lippa and Dolle, {Roland E.}",
note = "Publisher Copyright: {\textcopyright} 2016 American Chemical Society.",
year = "2016",
month = apr,
day = "14",
doi = "10.1021/acsmedchemlett.5b00368",
language = "English",
volume = "7",
pages = "374--378",
journal = "ACS Medicinal Chemistry Letters",
issn = "1948-5875",
number = "4",
}