ArticleJournal of medicinal chemistry2018
Alkylated Piperazines and Piperazine-Azole Hybrids as Antifungal Agents.
Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed.
- Synthesis, molecular docking and biological activity assessment of novel 1,3,4-oxadiazole derivatives as broad-spectrum antifungal candidates.RSC advances · 2026Article
- Triazoles as enzyme inhibitors: synthetic advances, mechanism of action, molecular docking studies and structure-activity relationships.Molecular diversity · 2026Review
- Advances in Piperazine-based Compounds for Antimicrobial Drug Development: Design, SAR, and Therapeutic Potential.Current drug research reviews · 2026Review
- Comprehensive insights into the role of nanocarriers in advancing azole-based ocular therapeutics.RSC advances · 2025Review
- New Generation Modified Azole Antifungals against Multidrug-ResistantJournal of medicinal chemistry · 2025Article
- Piperazine-Substituted Pyranopyridines Exhibit Antiproliferative Activity and Act as Inhibitors of HBV Virion Production.International journal of molecular sciences · 2025Article
- Design and synthesis of pyrrolo[2,3-d]pyrimidine linked hybrids as α-amylase inhibitors: molecular docking, MD simulation, ADMET and antidiabetic screening.Molecular diversity · 2024Article
- New thymol-derived triazole exhibits promising activity against Trichophyton rubrum.Brazilian journal of microbiology : [publication of the Brazilian Society for Microbiology] · 2024Article
- Catalytic Tetrazole Synthesis via [3+2] Cycloaddition of NaNACS omega · 2024Article
- Aspergillus flavus pangenome (AflaPan) uncovers novel aflatoxin and secondary metabolite associated gene clusters.BMC plant biology · 2024Article
- Building Up a Piperazine Ring from a Primary Amino Group via Catalytic Reductive Cyclization of Dioximes.International journal of molecular sciences · 2023Article
- Discovery and development of novel substituted monohydrazides as potent antifungal agents.RSC medicinal chemistry · 2023Article
- Anti-virulence activity of novel (1-heteroaryloxy-2-hydroxypropyl)- phenylpiperazine derivatives against both wild-type and clinical drug-resistant Candida albicans strains.Microbial biotechnology · 2023Article
- New Peptide Based Fluconazole Conjugates with Expanded Molecular Targets.Pharmaceutics · 2022Article
- Identification of a novel SPT inhibitor WXP-003 by docking-based virtual screening and investigation of its anti-fungi effect.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Design, Synthesis, andACS omega · 2021Article
- New 1,2,3-Triazole-Appended Bis-pyrazoles: Synthesis, Bioevaluation, and Molecular Docking.ACS omega · 2021Article
- Artificial Intelligence-GuidedACS omega · 2021Article
- Broad-Spectrum Antifungal Agents: Fluorinated Aryl- and Heteroaryl-Substituted Hydrazones.ChemMedChem · 2021Article
- DABCO bond cleavage for the synthesis of piperazine derivatives.RSC advances · 2019Review
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
The extensive use of fluconazole (FLC) and other azole drugs has caused the emergence and rise of azole-resistant fungi. The fungistatic nature of FLC in combination with toxicity concerns have resulted in an increased demand for new azole antifungal agents. Herein, we report the synthesis and antifungal activity of novel alkylated piperazines and alkylated piperazine-azole hybrids, their time-kill studies, their hemolytic activity against murine erythrocytes, as well as their cytotoxicity against mammalian cells. Many of these molecules exhibited broad-spectrum activity against all tested fungal strains, with excellent minimum inhibitory concentration (MIC) values against non-albicans Candida and Aspergillus strains. The most promising compounds were found to be less hemolytic than the FDA-approved antifungal agent voriconazole (VOR). Finally, we demonstrate that the synthetic alkylated piperazine-azole hybrids do not function by fungal membrane disruption, but instead by disruption of the ergosterol biosynthetic pathway via inhibition of the 14α-demethylase enzyme present in fungal cells.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.