Synthesis and application of fluorescently labeled monocyclic thio-beta-lactam derivatives.

摘要

Novel methodologies for the synthesis of fluorescently labeled monobactam derivatives were developed and explored. Two separate beta-lactam derivatives, 4-(4 aminophenylthio)azetidin-2-one and 4-phenylsulflanyl-azetidin-2-one were labeled with several combinations of fluorophores and electron withdrawing groups allowing for these drugs to be observed within a living bacterial cell. These drugs have shown considerable antimicrobial activity, but are not classified as beta-lactamase inhibitors or substrates. Observation of the drugs in vivo will provide valuable information as to the molecular targets and specific mechanism of antimicrobial action of these compounds.