This review provides a historical overview of the analog based drug discovery of miconazole and its congeners, and is focused on marketed azole antifungals bearing the generic suffix "conazole". The antifungal activity of miconazole, one of the first broad-spectrum antimycotic agents has been mainly restricted to topical applications. The attractive in vitro antifungal spectrum was a starting point to design more potent and especially orally active antifungal agents such as ketoconazole, itraconazole, posaconazole, fluconazole and voriconazole. The chemistry, in vitro and in vivo antifungal activity, pharmacology, and clinical applications of these marketed conazoles has been described.
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http://dx.doi.org/10.3390/molecules15064129 | DOI Listing |
AMB Express
January 2025
Department of Agricultural Microbiology, Faculty of Agriculture, Ain Shams University, P.O. Box 68, Cairo, 11241, Egypt.
The increasing demand for natural alternatives to synthetic fungicides has prompted research into natural products like essential oils for postharvest disease management. This study investigated the antifungal, antioxidant, cytotoxic, and genotoxic potential of essential oil mixtures derived from oregano, rosemary, and mint against Penicillium digitatum, the predominant fungal pathogen causing green mold in orange fruits. P.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
Nanotechnology Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 1416634793, Iran; Wound Care Solution, Nano Fanavaran Narin Teb Co., Tehran, P.O. Box 19177-53531, Iran; Physical Chemistry I, Department of Chemistry and Biology & Research Center of Micro and Nanochemistry and Engineering (Cμ), University of Siegen, 57076 Siegen, Germany. Electronic address:
This study reports the development of a highly absorbent Chitosan (CS)/Tannic Acid (TA) sponge, synthesized via chemical cross-linking with Epichlorohydrin (ECH) and integrated with zinc oxide nanoparticles (ZnO NPs) as a novel hemostatic anti-infection agent. The chemical properties of the sponges were characterized using Fourier-transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), thermogravimetric analysis (TGA), and zeta potential measurements. Morphological and elemental analyses conducted through scanning electron microscopy (SEM) and energy-dispersive X-ray spectroscopy (EDAX) revealed a uniform distribution of ZnO NPs, with particle sizes below 20 nm.
View Article and Find Full Text PDFInt J Biol Macromol
January 2025
Catalytic Applications Laboratory, Department of Chemistry, School of Basic Sciences, Faculty of Science, Manipal University Jaipur, Dehmi Kalan, Jaipur 303007, Rajasthan, India. Electronic address:
In the present study, biopolymeric Schiff base (SB) ligands were synthesized from chitosan and isatin. Consequently, their earth abundant transition metal complexes of cobalt and copper were synthesized. All compounds were extensively characterized using FTIR and UV spectroscopy, thermo-gravimetric (TG) analysis, X-ray powder diffraction (XRD) and FESEM (field emission scanning electron microscopy).
View Article and Find Full Text PDFJ Mater Chem B
January 2025
Drug Delivery, Disposition, and Dynamics Theme, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Pde, Parkville, VIC, 3052, Australia.
Infections caused by fungal pathogens are a global health problem, and have created an urgent need for new antimicrobial strategies. This report details the synthesis of lipidated 2-vinyl-4,4-dimethyl-5-oxazolone (VDM) oligomers an optimized Cu(0)-mediated reversible-deactivation radical polymerization (RDRP) approach. Cholesterol-Br was used as an initiator to synthesize a library of oligo-VDM (degree of polymerisation = 5, 10, 15, 20, and 25), with an α-terminal cholesterol group.
View Article and Find Full Text PDFJ Med Chem
January 2025
College of Animal Science and Technology, Northeast Agricultural University, Harbin 150030, P. R. China.
infection is a major public health problem, exacerbated by the emergence of drug-resistant fungi with the widespread use of antifungal drugs. Therefore, the development of novel antifungal drugs for drug-resistant infections is crucial. We constructed a series of dendritic antifungal peptides (AFPs) with different chain lengths of fatty acids as hydrophobic ends and 2 or 3 protease-stable repeats (Arg-Pro) as dendritic peptide branches.
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