调节碳青霉烯类和二氮杂双环辛烷类对结核分枝杆菌选择性活性的特异性。
Modulation of the Specificity of Carbapenems and Diazabicyclooctanes for Selective Activity against Mycobacterium tuberculosis.
机构信息
INSERM UMR-S 1138, Centre de Recherche des Cordeliers, Sorbonne Université, Université Paris Cité, Paris, France.
Université Paris Cité, Faculté de Santé, UFR de Médecine, Paris, France.
出版信息
Antimicrob Agents Chemother. 2022 Sep 20;66(9):e0235721. doi: 10.1128/aac.02357-21. Epub 2022 Aug 9.
Abstract
Treatment of multidrug-resistant tuberculosis with combinations of carbapenems and β-lactamase inhibitors carries risks for dysbiosis and for the development of resistances in the intestinal microbiota. Using Escherichia coli producing carbapenemase KPC-2 as a model, we show that carbapenems can be modified to obtain drugs that are inactive against E. coli but retain antitubercular activity. Furthermore, functionalization of the diazabicyclooctanes scaffold provided drugs that did not effectively inactivate KPC-2 but retained activity against Mycobacterium tuberculosis targets.
摘要
碳青霉烯类药物与β-内酰胺酶抑制剂联合治疗耐多药结核病存在肠道菌群失调和产生耐药性的风险。本研究以产生碳青霉烯酶 KPC-2 的大肠杆菌为模型，表明可以对碳青霉烯类药物进行修饰，得到对大肠杆菌无活性但保留抗结核活性的药物。此外，二氮杂双环辛烷骨架的功能化提供了一些药物，这些药物不能有效灭活 KPC-2，但对结核分枝杆菌靶标仍具有活性。
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