During our efforts to develop new antifungal agents, a number of hybrid molecules containing furanones and fluconazole pharmacophores were designed and synthesized. The new chemical entities thus synthesized were tested for their potential as antifungal agents against various fungal strains and it was observed that the compounds with general structure 7 were potent inhibitors of Candida albicans ATCC 24433, Candida glabrata ATCC 90030, Candida tropicalis ATCC 750 and Candida neoformans ATCC 34664 while the fluconazole analogues 12 exhibited antifungal activity against Candida albicans ATCC 24433 and Candida glabrata ATCC 90030. The structure-activity relationship for these compounds is discussed. The synthetic strategies used in the present work have potential to prepare a large number of compounds for further refinement of structures to obtain molecules suitable for development as antifungal drugs.
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http://dx.doi.org/10.1016/j.bmcl.2011.06.022 | DOI Listing |
Macromol Biosci
January 2025
Cluster for Advanced Macromolecular Design (CAMD) and Australian Centre for NanoMedicine (ACN), School of Chemical Engineering, UNSW, Sydney, NSW, 2052, Australia.
Invasive fungal infections cause over 3.7 million deaths worldwide annually, underscoring the critical need for new antifungal agents. Developing selective antifungal agents is challenging due to the shared eukaryotic nature of both fungal and mammalian cells.
View Article and Find Full Text PDFUnlabelled: Despite recent advances, the regulation of anticancer and antimicrobial bioactive compound (AABC) production by leukocytes remains poorly understood. Here, we demonstrate that inactivation of the DNA- and RNA-based Teazeled receptors of the Universal Receptive System in human leukocytes generated so called "Leukocyte-Tells," which showed enhanced AABC production. Comprehensive analysis of the AABCs produced by Leukocyte-Tells based on LC/MS identified 707 unique or differentially produced peptide or non-peptide metabolites.
View Article and Find Full Text PDFFront Immunol
December 2024
Department of Ophthalmology, The Second Hospital of Jilin University, Changchun, Jilin, China.
The treatment of fungal keratitis(FK) remains challenging due to delayed fungal detection and the limited effectiveness of antifungal drugs. Fungal infection can activate both innate and adaptive immune responses in the cornea. Fungi stimulate the production of oxidative stress-related biomarkers and mediate the infiltration of neutrophils, macrophages, and T cells.
View Article and Find Full Text PDFRSC Adv
January 2025
Botany and Microbiology Department, Faculty of Science, Al-Azhar University Nasr City Cairo 11884 Egypt
In this study, a nanocomposite based on copper oxide-zinc oxide nanoparticles and Gum Arabic (GA@CuO-ZnO nanocomposite) was successfully synthesized using green method. Characterization results revealed that the prepared nanocomposite appeared at the nanoscale level, showed excellent dispersion, and formed stable colloidal nano-solutions. The bimetallic GA@CuO-ZnO nanocomposite was evaluated for its anticancer, antibacterial, and antifungal properties.
View Article and Find Full Text PDFACS Appl Mater Interfaces
January 2025
Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, 744 Motooka, Fukuoka 819-0395, Japan.
The rising incidence of fungal infections, compounded by the emergence of severe antifungal resistance, has resulted in an urgent need for innovative antifungal therapies. We developed an antifungal protein-based formulation as a topical antifungal agent by combining an artificial lipidated chitin-binding domain of antifungal chitinase (LysM-lipid) with recently developed ionic liquid-in-oil microemulsion formulations (MEFs). Our findings demonstrated that the lipid moieties attached to LysM and the MEFs effectively disrupted the integrity of the stratum corneum in a mouse skin model, thereby enhancing the skin permeability of the LysM-lipids.
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