Microbial phosphorylation of the OA-6129 group of carbapenem compounds.
The OA-6129 group of carbapenem antibiotics were phosphorylated with ATP by Brevibacterium ammoniagenes at the primary hydroxyl group of the C-3 pantetheinyl side chain. The phosphorylation resulted in the reduced antimicrobial activity against some Gram-positive bacteria, and the improved activity against some Gram-negative microbes. The increased resistance of the OA-6129 carbapenems due to phosphorylation was significant to mouse renal dehydropeptidase and moderate to the human enzyme. OA-6129A and B2 phosphates were found to be unsusceptible to A933 acylase, while OA-6129A and B2 were depantothenylated.
D001419:Bacteria / Q000187:drug effects; D001951:Brevibacterium / Q000378:metabolism*; D004150:Dipeptidases / Q000494:pharmacology; D004355:Drug Stability; D010766:Phosphorylation; D013845:Thienamycins / Q000378:metabolism* / Q000494:pharmacology
D013845:Thienamycins; C036499:OA 6129C; C036497:OA 6129A; C036498:OA 6129B(1); C041410:OA 6129D; C041411:OA 6129E; D004150:Dipeptidases