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Design, Synthesis, and Biological Activity of New Triazole and Nitro-Triazole Derivatives as Antifungal Agents

1
Department of Medicinal Chemistry, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz 7146864685, Iran
2
Department of Medical Mycology and Parasitology, School of Medicine, Shiraz University of Medical Sciences, Shiraz 7134845794, Iran
3
Department of Medicinal Chemistry, School of Pharmacy, Kerman University of Medical Sciences, Kerman 7616911319, Iran
*
Author to whom correspondence should be addressed.
Molecules 2017, 22(7), 1150; https://doi.org/10.3390/molecules22071150
Received: 17 June 2017 / Revised: 6 July 2017 / Accepted: 7 July 2017 / Published: 10 July 2017
In this study two series of fluconazole derivatives bearing nitrotriazole (series A) or piperazine ethanol (series B) side chain were designed and synthesized and then docked in the active site of lanosterol 14α-demethylase enzyme (1EA1) using the Autodock 4.2 program (The scripps research institute, La Jolla, CA, USA). The structures of synthesized compound were confirmed by various methods including elemental and spectral (NMR, CHN, and Mass) analyses. Then antifungal activities of the synthesized compound were tested against several natural and clinical strains of fungi using a broth microdilution assay against several standard and clinical fungi. Nitrotriazole derivatives showed excellent and desirable antifungal activity against most of the tested fungi. Among the synthesized compounds, 5ad and 5g, possessing nitrotriazole moiety, showed maximum antifungal activity, in particular against several fluconazole-resistant fungi. View Full-Text
Keywords: fluconazole; synthesis; antifungal; lanosterol 14α-demethylase; docking; nitrotriazole fluconazole; synthesis; antifungal; lanosterol 14α-demethylase; docking; nitrotriazole
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MDPI and ACS Style

Sadeghpour, H.; Khabnadideh, S.; Zomorodian, K.; Pakshir, K.; Hoseinpour, K.; Javid, N.; Faghih-Mirzaei, E.; Rezaei, Z. Design, Synthesis, and Biological Activity of New Triazole and Nitro-Triazole Derivatives as Antifungal Agents. Molecules 2017, 22, 1150.

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