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抗疟疾药物甲氟喹类似物具有广谱抗真菌活性,并在播散性感染模型中有效。

Analogs of the anti-malaria drug mefloquine have broad-spectrum antifungal activity and are efficacious in a model of disseminated infection.

机构信息

Department of Chemistry, School of Science and Engineering, Saint Louis University, Saint Louis, Missouri, USA.

Department of Pediatrics, Carver College of Medicine, University of Iowa, Iowa City, Iowa, USA.

出版信息

Antimicrob Agents Chemother. 2024 Nov 6;68(11):e0130124. doi: 10.1128/aac.01301-24. Epub 2024 Oct 4.

Abstract

Only three classes of antifungal drugs are currently in clinical use. Here, we report that derivatives of the malarial drug mefloquine have broad-spectrum antifungal activity including difficult-to-treat molds and endemic fungi. Pharmacokinetic and efficacy studies of NSC-4377 indicate that it penetrates the central nervous system and is active against . These data strongly support the further development of mefloquine analogs as a potentially new class of antifungal molecules.

摘要

目前,临床上仅有三类抗真菌药物。在此,我们报告称,抗疟药物甲氟喹的衍生物具有广谱抗真菌活性,包括难以治疗的霉菌和地方性真菌。NSC-4377 的药代动力学和疗效研究表明,它能穿透中枢神经系统,并对有效。这些数据有力地支持了将甲氟喹类似物进一步开发为一种潜在的新型抗真菌分子。

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本文引用的文献

1
Clinical Mycology Today: Emerging Challenges and Opportunities.《今日临床真菌学:新出现的挑战与机遇》
Open Forum Infect Dis. 2024 Jun 27;11(7):ofae363. doi: 10.1093/ofid/ofae363. eCollection 2024 Jul.
2
Drug repurposing for bacterial infections.用于细菌感染的药物重新利用。
Prog Mol Biol Transl Sci. 2024;207:1-21. doi: 10.1016/bs.pmbts.2024.03.031. Epub 2024 May 11.
4
Synthesis and Antifungal Activity of Stereoisomers of Mefloquine Analogs.甲氟喹类似物立体异构体的合成及其抗真菌活性
ACS Med Chem Lett. 2024 May 1;15(6):822-827. doi: 10.1021/acsmedchemlett.4c00031. eCollection 2024 Jun 13.
6
Repurposing and optimization of drugs for discovery of novel antifungals.药物再利用和优化用于发现新型抗真菌药物。
Drug Discov Today. 2022 Jul;27(7):2008-2014. doi: 10.1016/j.drudis.2022.04.021. Epub 2022 Apr 27.

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