Amidino benzimidazole inhibitors of bacterial two-component systems.
Amidino benzimidazoles have been identified as inhibitors of the bacterial KinA/Spo0F two-component system (TCS). Many of these inhibitors exhibit good in vitro antibacterial activity against a variety of susceptible and resistant Gram-positive organisms. The moiety at the 2-position of the benzimidazole was extensively modified. In addition, the regioisomeric benzoxazoles, heterocyclic replacements for the benzimidazole, have been synthesized and their activity against the TCS evaluated.
Weidner-Wells
M A
MA
Drug Discovery, The R. W. Johnson Pharmaceutical Research Institute, 1000 Route 202, Raritan, NJ 08869, USA.
Ohemeng
K A
KA
Nguyen
V N
VN
Fraga-Spano
S
S
Macielag
M J
MJ
Werblood
H M
HM
Foleno
B D
BD
Webb
G C
GC
Barrett
J F
JF
Hlasta
D J
DJ
D000578:Amidines / Q000138:chemical synthesis / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D020650:Combinatorial Chemistry Techniques; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000502:physiology; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases; D015398:Signal Transduction / Q000187:drug effects
D000578:Amidines; D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; C080951:Spo0F protein, Bacillus subtilis; C075521:kinA protein, Bacillus subtilis; D011494:Protein Kinases