Acetophenones with selective antimycobacterial activity.
OBJECTIVE
Mycobacteria are a serious cause of infections in humans, with limited treatment options, as no new antibiotics have been developed against mycobacteria since the 1960s. In this study, the antimycobacterial activity of a small library of acetophenone (AP) compounds was analysed.


RESULTS
Twenty-three AP derivatives were examined for activity against mycobacteria using a microbroth assay. The compounds were bacteriostatic, with the most effective (cyclohexylacetophenone and piperidinoacetophenone) having minimal inhibitory concentrations of 246 microM. Active compounds tended to be more hydrophobic, and may work by alkylation of as yet undetermined intracellular target protein(s). Cytotoxicity against eukaryotic cells was also determined and appears to be unrelated to the bacteriostatic activity.


CONCLUSIONS
AP may serve as a novel group of useful therapeutics against the mycobacteria.
Rajabi
L
L
Department of Biological Sciences and Border Biomedical Research Center, The University of Texas at El Paso, El Paso, TX 79968, USA.
Courreges
C
C
Montoya
J
J
Aguilera
R J
RJ
Primm
T P
TP
D000098:Acetophenones / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009161:Mycobacterium / Q000187:drug effects*
D000098:Acetophenones; D000900:Anti-Bacterial Agents