Synthesis, in vitro and in vivo antibacterial activity of 7-(7-methyl-2,5-diazabicyclo[2.2.1]heptane)naphthyridone derivatives as analogs of BMY 40062

The synthesis and the antimicrobial activities of chiral (1R,4R,7S)- and (1S,4S,7S)-[7-methyl-2,5-diazabicyclo[2.2.1]-heptan-2-yl] analogs of BMY 40062 are reported. The new derivatives have been found to be less active in vitro but as active in vivo (im) than BMY 40062. The 1R,4R,7S substituent seems promising for the design of powerful new antibiotics.