N1-phenyl substituted 4-quinolones of tuberculostatic activity.
Various different substituted N1-phenyl-6-fluoro-7-piperazinyl-4-quinolone 3-carboxylates and the diazoniumtetrafluoroborate of sparfloxacin were tested for their ability to inhibit the growth of various Mycobacterium strains of different origin. The N1-p-hydroxylphenyl substituted compound 22 and the methoxyphenyl substituted compound missing the piperazine ring 12 were identified as promising candidates for the further development of an improved treatment of tuberculosis. In addition, compound 22 and the N1-p-fluorophenyl substituted analogue 4 were found to be active against Mycobacterium avium, which is often isolated from patients suffering from AIDS.
Holzgrabe
U
U
Institut für Pharmazie und Lebensmittelchemie, Universität Würzburg, Germany. U.Holzgrabe@pharmazie.uni-wuerzburg.de
Steinert
M
M
D042462:4-Quinolones; D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002522:Chlorocebus aethiops; D006801:Humans; D008826:Microbial Sensitivity Tests; D015269:Mycobacterium avium Complex / Q000187:drug effects; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014709:Vero Cells
D042462:4-Quinolones; D000890:Anti-Infective Agents; D000995:Antitubercular Agents