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

IF 4.1 2区 医学 Q2 MICROBIOLOGY Antimicrobial Agents and Chemotherapy Pub Date : 2024-10-04 DOI:10.1128/aac.01301-24
Soumitra Guin, Marhiah C Montoya, Xiaoyu Wang, Robert Zarnowski, David R Andes, Marvin J Meyers, Noelle S Williams, Damian J Krysan
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引用次数: 0

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 Candida auris in vivo. These data strongly support the further development of mefloquine analogs as a potentially new class of antifungal molecules.

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抗疟疾药物甲氟喹的类似物具有广谱抗真菌活性,对播散性念珠菌感染模型有效。
目前临床上使用的抗真菌药物只有三类。在此,我们报告了疟疾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真菌。NSC-4377 的药代动力学和药效研究表明,它能穿透中枢神经系统,对体内的白色念珠菌具有活性。这些数据有力地支持了甲氟喹类似物作为一类潜在的新型抗真菌分子的进一步发展。
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来源期刊
CiteScore
10.00
自引率
8.20%
发文量
762
审稿时长
3 months
期刊介绍: Antimicrobial Agents and Chemotherapy (AAC) features interdisciplinary studies that build our understanding of the underlying mechanisms and therapeutic applications of antimicrobial and antiparasitic agents and chemotherapy.
期刊最新文献
Analogs of the anti-malaria drug mefloquine have broad-spectrum antifungal activity and are efficacious in a model of disseminated Candida auris infection. High frequency of acquired virulence factors in carbapenemase-producing Klebsiella pneumoniae isolates from a large German university hospital, 2013-2021. Impact of porin deficiency on the synergistic potential of colistin in combination with β-lactam/β-lactamase inhibitors against ESBL- and carbapenemase-producing Klebsiella pneumoniae. Relative inhibitory activities of newly developed diazabicyclooctanes, boronic acid derivatives, and penicillin-based sulfone β-lactamase inhibitors against broad-spectrum AmpC β-lactamases. Oral oxaborole MRX-5 exhibits efficacy against pulmonary Mycobacterium abscessus in mouse.
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