Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.
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.
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Jason B
JB
Cross
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Jing
J
Zhang
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Qingyi
Q
Yang
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Michael F
MF
Mesleh
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Jan Antoinette C
JA
Romero
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Bin
B
Wang
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Doug
D
Bevan
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Katherine M
KM
Poutsiaka
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Felix
F
Epie
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Terence
T
Moy
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Anu
A
Daniel
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Joseph
J
Shotwell
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Brian
B
Chamberlain
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Nicole
N
Carter
Evotec U.K., Ltd. , 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, United Kingdom.
Ole
O
Andersen
Evotec U.K., Ltd. , 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, United Kingdom.
John
J
Barker
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
M Dominic
MD
Ryan
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Chester A
CA
Metcalf
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Jared
J
Silverman
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Kien
K
Nguyen
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Blaise
B
Lippa
Cubist Pharmaceuticals, Inc. , 65 Hayden Avenue, Lexington, Massachusetts 02421, United States.
Roland E
RE
Dolle
Antibacterials; DNA gyrase B; fragment-based drug design; structure-based drug design