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Chemistry. 2021 Feb 15;27(10):3542-3551. doi: 10.1002/chem.202004831. Epub 2021 Jan 21.
2
New β-Lactam-β-Lactamase Inhibitor Combinations.新型β-内酰胺类-β-内酰胺酶抑制剂复方制剂
Clin Microbiol Rev. 2020 Nov 11;34(1). doi: 10.1128/CMR.00115-20. Print 2020 Dec 16.
3
Ceftazidime-Avibactam Resistance Mediated by the NY Substitution in Various AmpC β-Lactamases.各种 AmpC β-内酰胺酶中 NY 取代导致头孢他啶-阿维巴坦耐药。
Antimicrob Agents Chemother. 2020 May 21;64(6). doi: 10.1128/AAC.02311-19.
4
Diazabicyclooctane Functionalization for Inhibition of β-Lactamases from Enterobacteria.氮杂二环辛烷的功能化用于抑制肠杆菌属的β-内酰胺酶。
J Med Chem. 2020 May 28;63(10):5257-5273. doi: 10.1021/acs.jmedchem.9b02125. Epub 2020 May 14.
5
Drug-associated adverse events in the treatment of multidrug-resistant tuberculosis: an individual patient data meta-analysis.药物相关不良事件在耐多药结核病治疗中的作用：一项个体患者数据荟萃分析。
Lancet Respir Med. 2020 Apr;8(4):383-394. doi: 10.1016/S2213-2600(20)30047-3. Epub 2020 Mar 17.
6
Combination of Amino Acid Substitutions Leading to CTX-M-15-Mediated Resistance to the Ceftazidime-Avibactam Combination.导致 CTX-M-15 介导的对头孢他啶-阿维巴坦组合耐药的氨基酸取代的组合。
Antimicrob Agents Chemother. 2018 Aug 27;62(9). doi: 10.1128/AAC.00357-18. Print 2018 Sep.
7
Synthesis of Avibactam Derivatives and Activity on β-Lactamases and Peptidoglycan Biosynthesis Enzymes of Mycobacteria.阿维巴坦衍生物的合成及其对分枝杆菌β-内酰胺酶和肽聚糖生物合成酶的活性。
Chemistry. 2018 Jun 7;24(32):8081-8086. doi: 10.1002/chem.201800923. Epub 2018 May 14.
8
Meropenem-clavulanate for drug-resistant tuberculosis: a follow-up of relapse-free cases.美罗培南-克拉维酸治疗耐药结核病：无复发病例的随访。
Int J Tuberc Lung Dis. 2018 Jan 1;22(1):34-39. doi: 10.5588/ijtld.17.0352.
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Peptidoglycan Cross-Linking Activity of l,d-Transpeptidases from Clostridium difficile and Inactivation of These Enzymes by β-Lactams.艰难梭菌 l,d-转肽酶的肽聚糖交联活性及β-内酰胺类药物对这些酶的抑制作用。
Antimicrob Agents Chemother. 2017 Dec 21;62(1). doi: 10.1128/AAC.01607-17. Print 2018 Jan.
10
Impaired Inhibition by Avibactam and Resistance to the Ceftazidime-Avibactam Combination Due to the DY Substitution in the KPC-2 β-Lactamase.因KPC-2 β-内酰胺酶中的DY取代导致阿维巴坦抑制作用受损及对头孢他啶-阿维巴坦联合制剂耐药
Antimicrob Agents Chemother. 2017 Jun 27;61(7). doi: 10.1128/AAC.00451-17. Print 2017 Jul.

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.

DOI:10.1128/aac.02357-21
PMID:35943263
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9487530/
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。