jm5b00961_si_001.csv (2.55 kB)
Discovery of Azaindole Ureas as a Novel Class of Bacterial Gyrase B Inhibitors
dataset
posted on 2015-11-12, 00:00 authored by Jing Zhang, Qingyi Yang, Jason B. Cross, Jan Antoinette
C. Romero, Katherine M. Poutsiaka, Felix Epie, Douglas Bevan, Bin Wang, Yanzhi Zhang, Ajit Chavan, Xin Zhang, Terence Moy, Anu Daniel, Kien Nguyen, Brian Chamberlain, Nicole Carter, Joseph Shotwell, Jared Silverman, Chester A. Metcalf, Dominic Ryan, Blaise Lippa, Roland E. DolleThe
emergence and spread of multidrug resistant bacteria are widely
believed to endanger human health. New drug targets and lead compounds
exempt from cross-resistance with existing drugs are urgently needed.
We report on the discovery of azaindole ureas as a novel class of
bacterial gyrase B inhibitors and detail the story of their evolution
from a de novo design hit based on structure-based
drug design. These inhibitors show potent minimum inhibitory concentrations
against fluoroquinolone resistant MRSA and other
Gram-positive bacteria.
