SAR studies of diaryltriazoles against bacterial two-component regulatory systems and their antibacterial activities.
A series of diaryltriazole analogs was discovered to inhibit bacterial two-component regulatory systems in our primary assays, KinA/Spo0F and NRII/NRI. They also showed inhibitory activity in whole cell mechanism-based assays, and they possessed potent activities against several strains of Gram-positive pathogenic bacteria in the standard MIC broth assay.
Sui
Z
Z
R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, USA.
Guan
J
J
Hlasta
D J
DJ
Macielag
M J
MJ
Foleno
B D
BD
Goldschmidt
R M
RM
Loeloff
M J
MJ
Webb
G C
GC
Barrett
J F
JF
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D014230:Triazoles