TABLE 1.

Chemical structure and activities of naphthyridine-type ribosome inhibitors

CompoundStructureS. pneumoniae in vitro translation (IC50 [μM])Effect of A1492/3 footprinting sitesaCompetition with [3H]A-424902 for binding to Phe-tRNAPheb
A-72310 Embedded Image 5+++
A-69234514+NT
A-4249021.6++++
A-3588161++++
A-3625055++++
A-4383019.2
A-548501>200NT
  • a “+++”, “++”, and “+” denote strong (IC50 < 20 μM), moderate (IC50 = 21 to 100 μM), and weak (IC50 > 100 μM) effects, respectively, on the increase in tRNA protection.

  • b “+” and “−” denote positive and negative competition effects, respectively. NT, not tested.