New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
The synthesis, structure, and biological evaluation of a series of novel rifamycin derivatives, Rifastures (RFA) with potent anti-tuberculosis activity are presented. Some of these derivatives showed higher in vitro activity than rifabutin and rifampicin against not only Mycobacterium tuberculosis strains but also against MAC and Mycobacterium kansasii.
Barluenga
José
J
Instituto Universitario de Química Organometálica Enrique Moles, Unidad Asociada al CSIC, Universidad de Oviedo, C/ Julián Clavería, 8, 33006 Oviedo, Spain. barluenga@uniovi.es
Aznar
Fernando
F
García
Ana-Belén
AB
Cabal
María-Paz
MP
Palacios
Juan J
JJ
Menéndez
María-Angela
MA
D000904:Antibiotics, Antitubercular / Q000138:chemical synthesis / Q000494:pharmacology*; D004352:Drug Resistance, Microbial; D008826:Microbial Sensitivity Tests; D015269:Mycobacterium avium Complex / Q000187:drug effects*; D019909:Mycobacterium kansasii / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D017828:Rifabutin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D012293:Rifampin / Q000494:pharmacology
D000904:Antibiotics, Antitubercular; D017828:Rifabutin; D012293:Rifampin