ArticleBioorganic & medicinal chemistry2018
Novel fluconazole derivatives with promising antifungal activity.
Article in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 33 citations in OpenAlex.
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- Discovery and development of novel substituted monohydrazides as potent antifungal agents.RSC medicinal chemistry · 2023Article
- Ketoconazole-Loaded Cationic Nanoemulsion:ACS omega · 2022Article
- Chitosan-Based Films with 2-Aminothiophene Derivative: Formulation, Characterization and Potential Antifungal Activity.Marine drugs · 2022Article
- Novel 1, 2, 4-Triazoles as Antifungal Agents.BioMed research international · 2022Review
- Design, Synthesis, andACS omega · 2021Article
- Broad-Spectrum Antifungal Agents: Fluorinated Aryl- and Heteroaryl-Substituted Hydrazones.ChemMedChem · 2021Article
- Iron Pathways and Iron Chelation Approaches in Viral, Microbial, and Fungal Infections.Pharmaceuticals (Basel, Switzerland) · 2020Review
- Fluconazole analogues with metal-binding motifs impact metal-dependent processes and demonstrate antifungal activity in Candida albicans.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2020Article
- Essential Oil-Based Design and Development of Novel Anti-Molecules (Basel, Switzerland) · 2020Article
- Pathogenesis and Clinical Relevance ofFrontiers in microbiology · 2020Review
- Biologically active metabolite(s) from haemolymph of red-headed centipede Scolopendra subspinipes possess broad spectrum antibacterial activity.AMB Express · 2019Article
- Differential Effects of Linkers on the Activity of Amphiphilic Tobramycin Antifungals.Molecules (Basel, Switzerland) · 2018Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The fungistatic nature and toxicity concern associated with the azole drugs currently on the market have resulted in an increased demand for new azole antifungal agents for which these problematic characteristics do not exist. The extensive use of azoles has resulted in fungal strains capable of resisting the action of these drugs. Herein, we report the synthesis and antifungal activity of novel fluconazole (FLC) analogues with alkyl-, aryl-, cycloalkyl-, and dialkyl-amino substituents. We evaluated their antifungal activity by MIC determination and time-kill assay as well as their safety profile by hemolytic activity against murine erythrocytes as well as cytotoxicity against mammalian cells. The best compounds from our study exhibited broad-spectrum activity against most of the fungal strains tested, with excellent MIC values against a number of clinical isolates. The most promising compounds were found to be less hemolytic than the least hemolytic FDA-approved azole antifungal agent voriconazole (VOR). Finally, we demonstrated that the synthetic alkyl-amino FLC analogues displayed chain-dependent fungal membrane disruption as well as inhibition of ergosterol biosynthesis as possible mechanisms of action.
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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.