Thiosemicarbazones of 2-acetylpyridine, 2-acetylquinoline, 1- and 3-acetylisoquinoline and related compounds as inhibitors of clinically significant bacteria in vitro.
Antibacterial activity of 64 thiosemicarbazones of 2-acetylpyridine, 2-acetylquinoline, 1- and 3-acetylisoquinoline and related compounds was determined by testing clinical isolates of ten bacterial genera, including some which were antibiotic resistant. Minimal inhibitory concentrations (MICs) of 0.016 to 0.125 microgram/ml were obtained with 26% of the compounds for Neisseria meningitidis and 0.002 to 0.25 microgram/ml with 19% of the compounds for N. gonorrhoeae. Staphylococcus aureus was inhibited in the MIC range of 0.062 to 0.5 microgram/ml by 34% of the thiosemicarbazones, whereas 26% inhibited Streptococcus faecalis with an MIC range of 0.25 to 1.0 microgram/ml. Less antibacterial activity was shown toward the Gram-negative bacilli, i.e., Pseudomonas, Klebsiella-Enterobacter, Shigella, Escherichia coli, Serratia marcescens and Proteus.
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis*; D001419:Bacteria / Q000187:drug effects*; D055598:Chemical Phenomena; D002621:Chemistry; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D007546:Isoquinolines; D011725:Pyridines; D011804:Quinolines; D013882:Thiosemicarbazones