The present invention relates to rifamycin 3-iminomethylenyl
(--CH.dbd.N--) derivatives having antimicrobial activities, including
activities against drug-resistant microorganisms. The claimed rifamycin
derivative has a rifamycin moiety covalently linked to a linker through
an iminomethylenyl (--CH.dbd.N--) group at the C-3 carbon of the
rifamycin moiety and the linker is, in turn, covalently linked to a
quinolone structure or its pharmacophore within the DNA gyrase and
topoisomerase IV inhibitor family. The inventive rifamycins are novel and
exhibit activity against both rifampin and ciprofloxacin-resistant
microorganisms.