The syntheses and anti-tuberculosis activity of quinolone-cephalosporin conjugates (1 and 2) are described. Both showed broad-spectrum antibacterial activity and significant anti-TB activity. The carbamate-linked quinolone-cephem 2 showed better antimycobacterial activity, including anti-TB activity, than the direct amine-linked quinolone-cephem 1, while quinolone-cephem 1 was slightly more effective against some Gram-negative bacterial strains.