The synthesis, in vitro antifungal evaluation and SAR studies of 101 compounds of the 4-aryl-, 4-alkyl-, 4-pyridyl or -quinolinyl-4-N-arylamino-1-butenes series and related compounds, are reported here. Active structures showed to inhibit (1,3)-beta-D-glucan and mainly chitin synthases, enzymes that catalyze the synthesis of the major fungal cell wall polymers.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/s0968-0896(02)00605-3 | DOI Listing |
J Med Chem
January 2025
The Center for Basic Research and Innovation of Medicine and Pharmacy (MOE), School of Pharmacy, Second Military Medical University (Naval Medical University), 325 Guohe Road, Shanghai 200433, China.
Invasive candidiasis has attracted global attention with a high incidence and mortality. Current antifungal drugs are limited by unfavorable therapeutic efficacy, significant hepatorenal toxicity, and the development of drug resistance. Herein, we designed the first generation of lanosterol 14α-demethylase (CYP51)/heat shock protein 90 (Hsp90) dual inhibitors on the basis of antifungal synergism.
View Article and Find Full Text PDFMycoses
January 2025
Department of Dermatology and Venereology, Peking University First Hospital, Beijing, China.
Background: Microsporum canis, a dermatophyte commonly associated with pets, is a leading cause of severe tinea capitis. The increasing prevalence of antifungal resistance among dermatophytes poses a significant global health challenge.
Objectives: This study aims to define the updated antifungal susceptibility profile of M.
Sci Rep
January 2025
Department of Biotechnology Engineering, NITTE (Deemed to be University), NMAM Institute of Technology, 574110, Karnataka, India.
Endophytes from medicinal plants are potential biocontrol agents against Fusarium oxysporum f. sp. cubense (Foc), which is the causative fungus of banana wilt disease.
View Article and Find Full Text PDFSci Rep
January 2025
Dental Health Department, College of Applied Medical Sciences, King Saud University, P.O. Box 10219, Riyadh, 11433, Saudi Arabia.
In this study, the endophytic fungus Coniothyrium chaingmaiense-KUMBMDBT-25 was isolated from the healthy stem of Euphorbia tirucalli, mass cultivated by submerged fermentation, and extracted using ethyl acetate as a solvent. The extract was subjected to GC-MS analysis. The synthesized Con-AgNPs were characterized through various bioanalytical methods.
View Article and Find Full Text PDFJ Photochem Photobiol B
December 2024
Anne Bates Leach Eye Center, Bascom Palmer Eye Institute, Department of Ophthalmology, University of Miami Miller School of Medicine, Miami, FL, United States of America; Ocular Microbiology Laboratory, Bascom Palmer Eye Institute, Department of Ophthalmology, University of Miami Miller School of Medicine, Miami, FL, United States of America.
Introduction: Fungal keratitis is a leading cause of corneal blindness, with current antifungal treatments having limited efficacy. One promising treatment modality is Rose Bengal (RB) photodynamic antimicrobial therapy (PDAT) that has shown mixed success against fungal keratitis. Therefore, there is a need to explore the antimicrobial efficacy of other green-light activated photosensitizers that have deep penetration in the cornea to combat the deep fungal infections, such as Erythrosin B (EB) and Eosin Y (EY).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!