Use of the chromosomal class A beta-lactamase of Mycobacterium fortuitum D316 to study potentially poor substrates and inhibitory beta-lactam compounds.
Sixteen different compounds usually considered beta-lactamase stable or representing potential beta-lactam inhibitors and inactivators were tested against the beta-lactamase produced by Mycobacterium fortuitum. The compounds exhibiting the most interesting properties were BRL42715, which was by far the best inactivator, and CGP31608 and ceftazidime, which were not recognized by the enzyme. These compounds thus exhibited adequate properties for fighting mycobacterial infections. Although cloxacillin, dicloxacillin, cefoxitin, and CP65207-2 exhibited poor inhibitory efficiency against the enzyme, they were also rather poor substrates and might be considered potential antimycobacterial agents. By contrast, CGP31523A and ceftamet were good substrates.
Galleni
M
M
Laboratory of Enzymology, University of Liège, Belgium.
Franceschini
N
N
Quinting
B
B
Fattorini
L
L
Orefici
G
G
Oratore
A
A
Frère
J M
JM
Amicosante
G
G
D000900:Anti-Bacterial Agents / Q000378:metabolism / Q000494:pharmacology*; D002876:Chromosomes, Bacterial / Q000201:enzymology*; D019818:Clavulanic Acid; D002969:Clavulanic Acids / Q000494:pharmacology; D007700:Kinetics; D007769:Lactams; D009161:Mycobacterium / Q000187:drug effects / Q000201:enzymology*; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism*; D047090:beta-Lactams
D000900:Anti-Bacterial Agents; D002969:Clavulanic Acids; D007769:Lactams; D065093:beta-Lactamase Inhibitors; D047090:beta-Lactams; C061593:C6-(N1-methyl-1,2,3-trazolylmethylene)penem; D019818:Clavulanic Acid; D001618:beta-Lactamases