UK-18,892: resistance to modification by aminoglycoside-inactivating enzymes.
UK-18,892, a new semisynthetic aminoglycoside, was active against bacteria possessing aminoglycoside-inactivating enzymes, with the exception of some known to possess AAC(6') or AAD(4') enzymes. This activity has been rationalized by using cell-free extracts of bacteria containing known inactivating enzymes, where it was shown that UK-18,892 was not a substrate for the APH(3'), AAD(2''), AAC(3), and AAC(2') enzymes. It was also demonstrated that UK-18,892 protected mice against lethal infections caused by organisms possessing aminoglycoside-inactivating enzymes.
D001419:Bacteria / Q000187:drug effects / Q000201:enzymology*; D004794:Enzyme Repression; D005839:Gentamicins / Q000494:pharmacology; D007612:Kanamycin / Q000031:analogs & derivatives* / Q000494:pharmacology; D007928:Lethal Dose 50
D005839:Gentamicins; D007612:Kanamycin