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Issue 47, 2019
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The synthesis of an antifungal 1,2,4-triazole drug and the establishment of a drug delivery system based on zeolitic imidazolate frameworks

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Abstract

Invasive fungal infections (IFIs) are deadly fungal infections with a high mortality rate, particularly in patients who have undergone prolonged use of chemotherapy drugs, transplant surgery and so on. Among them, Candida albicans has attracted great attention as an important pathogen. Triazoles such as voriconazole and fluconazole are considered to be some of the most effective and widely used antifungal drugs. However, the resistance of fungi to these drugs and the toxicity of triazoles to normal human cells are the main reasons for the difficulty of treating invasive fungal infections. In this paper, a novel trifluoromethyl-containing triazole compound, TPHMB, was designed and synthesized for the first time. The single crystal was obtained by the solution evaporation method, and its molecular structure was determined by a single crystal diffractometer. The activity against Candida albicans was detected (MIC90 = 8 μg ml−1). In addition, for the first time, we used the metal organic framework ZIF-8 to establish an effective, low-toxicity and pH-responsive antifungal drug delivery system with less side effects via reducing the non-specific aggregation in normal tissues and improving water solubility. Detailed material characterizations confirmed the successful encapsulation of TPHMB in the ZIF-8 matrix, which demonstrated good drug release at pH = 5; plate count was used to find the excellent synergy of ZIF-8 against Candida albicans. This study not only provides a reference for the development of new triazole drugs, but also helps develop an effective delivery system of such drugs in vivo to achieve an effective treatment of fungal infections.

Graphical abstract: The synthesis of an antifungal 1,2,4-triazole drug and the establishment of a drug delivery system based on zeolitic imidazolate frameworks

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Supplementary files

Article information


Submitted
27 Aug 2019
Accepted
03 Nov 2019
First published
04 Nov 2019

New J. Chem., 2019,43, 18823-18831
Article type
Paper

The synthesis of an antifungal 1,2,4-triazole drug and the establishment of a drug delivery system based on zeolitic imidazolate frameworks

S. Jiao, Y. Li, Z. Gao, R. Chen, Y. Wang and Z. Zou, New J. Chem., 2019, 43, 18823
DOI: 10.1039/C9NJ04432A

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