New long-acting 3-azinomethyl-rifamycins.
A number of basic 3-azinomethyl-rifamycins have been prepared. Their synthesis and antibacterial activity in vitro are reported, as well as the preliminary pharmacokinetic data. While the antimicrobial activity is comparable with that of rifampicin, serum levels in mice are much longer lasting. One of the compounds was selected for further studies.
T
T
Bruzzese
A
A
Cedro
E
E
Dell'Acqua
A
A
Di Nardo
A
A
Goi
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000378:metabolism; D001419:Bacteria / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D007700:Kinetics; D013058:Mass Spectrometry; D051379:Mice; D012293:Rifampin / Q000494:pharmacology; D012294:Rifamycins / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D012294:Rifamycins; D012293:Rifampin