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UK-18,892:对氨基糖苷类失活酶修饰具有抗性。

UK-18,892: resistance to modification by aminoglycoside-inactivating enzymes.

作者信息

Andrews R J, Brammer K W, Cheeseman H E, Jevons S

出版信息

Antimicrob Agents Chemother. 1978 Dec;14(6):846-50. doi: 10.1128/AAC.14.6.846.

Abstract

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.

摘要

UK-18892是一种新型半合成氨基糖苷类药物,对具有氨基糖苷类失活酶的细菌具有活性,但已知具有AAC(6')或AAD(4')酶的细菌除外。通过使用含有已知失活酶的细菌无细胞提取物,对这种活性进行了合理的解释,结果表明UK-18892不是APH(3')、AAD(2'')、AAC(3)和AAC(2')酶的底物。还证明了UK-18892能保护小鼠免受具有氨基糖苷类失活酶的生物体引起的致命感染。

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