Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
Antibacterials with a novel mechanism of action offer a great opportunity to combat widespread antimicrobial resistance. Bacterial DNA Gyrase is a clinically validated target. Through physiochemical property optimization of a pyrazolopyridone hit, a novel class of GyrB inhibitors were discovered. Guided by structure-based drug design, indazole derivatives with excellent enzymatic and antibacterial activity as well as great animal efficacy were discovered.
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Jing
J
Zhang
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Qingyi
Q
Yang
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Jan Antoinette C
JA
Romero
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Jason
J
Cross
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Bin
B
Wang
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Katherine M
KM
Poutsiaka
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Felix
F
Epie
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Douglas
D
Bevan
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Yuchuan
Y
Wu
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Terence
T
Moy
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Anu
A
Daniel
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Brian
B
Chamberlain
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Nicole
N
Carter
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Joseph
J
Shotwell
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Anu
A
Arya
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Vipul
V
Kumar
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Jared
J
Silverman
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Kien
K
Nguyen
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Chester A
CA
Metcalf
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Dominic
D
Ryan
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Blaise
B
Lippa
Cubist Pharmaceuticals Inc. , Lexington, Massachusetts 02421, United States.
Roland E
RE
Dolle
Antibacterial; GyrB; MRSA; indazole; topoisomerase