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Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design
DOI:
10.1021/acsmedchemlett.5b00368
Authors:
Jason B.
Cross
(Cubist Pharmaceuticals, Inc)
,
Jing
Zhang
(Cubist Pharmaceuticals, Inc)
,
Qingyi
Yang
(Cubist Pharmaceuticals, Inc)
,
Michael F.
Mesleh
(Cubist Pharmaceuticals, Inc)
,
Jan Antoinette C.
Romero
(Cubist Pharmaceuticals, Inc)
,
Bin
Wang
(Cubist Pharmaceuticals, Inc)
,
Doug
Bevan
(Cubist Pharmaceuticals, Inc)
,
Katherine M.
Poutsiaka
(Cubist Pharmaceuticals, Inc)
,
Felix
Epie
(Cubist Pharmaceuticals, Inc)
,
Terence
Moy
(Cubist Pharmaceuticals, Inc)
,
Anu
Daniel
(Cubist Pharmaceuticals, Inc)
,
Joseph
Shotwell
(Cubist Pharmaceuticals, Inc)
,
Brian
Chamberlain
(Cubist Pharmaceuticals, Inc)
,
Nicole
Carter
(Cubist Pharmaceuticals, Inc)
,
Ole
Andersen
(Evotec U.K., Ltd)
,
John
Barker
(Evotec U.K., Ltd)
,
M. Dominic
Ryan
(Cubist Pharmaceuticals, Inc)
,
Chester A.
Metcalf
(Cubist Pharmaceuticals, Inc)
,
Jared
Silverman
(Cubist Pharmaceuticals, Inc)
,
Kien
Nguyen
(Cubist Pharmaceuticals, Inc)
,
Blaise
Lippa
(Cubist Pharmaceuticals, Inc)
,
Roland E.
Dolle
(Cubist Pharmaceuticals, Inc)
Co-authored by industrial partner:
No
Type:
Journal Paper
Journal:
Acs Medicinal Chemistry Letters
State:
Published (Approved)
Published:
February 2016
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
Journal Keywords: Antibacterials; DNA gyrase B; fragment-based drug design; structure-based drug design
Subject Areas:
Medicine,
Biology and Bio-materials
Instruments:
I03-Macromolecular Crystallography
,
I04-1-Macromolecular Crystallography (fixed wavelength)
,
I04-Macromolecular Crystallography