Novel rifamycins. III. Synthesis and antibacterial activity of 3-amidino- and of 4-aminoimidazolo[4,5-c]rifamycin derivatives.
A number of semisynthetic rifamycin derivatives modified at position 3 and/or 4, belonging to general structures 2 and 4 (see Scheme 1), have been obtained. The synthesis and the biological activities of the new compounds are described. Compounds 4p and 4q display very good antimycobacterial activity in mice.
D000818:Animals; D001419:Bacteria / Q000187:drug effects; D005260:Female; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D012293:Rifampin / Q000633:toxicity; D012294:Rifamycins / Q000138:chemical synthesis* / Q000633:toxicity; D013329:Structure-Activity Relationship
D007202:Indicators and Reagents; D012294:Rifamycins; D012293:Rifampin